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  Subjects -> PHARMACY AND PHARMACOLOGY (Total: 554 journals)
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Journal Cover Saudi Pharmaceutical Journal
  [SJR: 0.552]   [H-I: 20]   [0 followers]  Follow
  This is an Open Access Journal Open Access journal
   ISSN (Print) 1319-0164
   Published by Elsevier Homepage  [3043 journals]
  • Pharmacovigilance system in Saudi Arabia

    • Authors: Thamir M. Alshammari; Mohammed Alshakka; Hisham Aljadhey
      Pages: 299 - 305
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): Thamir M. Alshammari, Mohammed Alshakka, Hisham Aljadhey
      Pharmacovigilance plays an important role in ensuring that patients are receiving safe drugs. In Saudi Arabia, Saudi Food and Drug Authority, health institutions, marketing authorization holders and healthcare professional are involved in pharmacovigilance activities regardless of the level of the involvement. Although pharmacovigilance is well established in developed nations and it is considered a new concept in Saudi Arabia. It is a collective effort from various stakeholders to make pharmacovigilance successful toward promoting safe and effective use of medicines among the population. However, the practice of pharmacovigilance still needs more attention especially from marketing authorization holders and healthcare professionals. The aim of this review was to describe the current situation of pharmacovigilance in Saudi Arabia and the activities that have been conducted by the stakeholders.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.09.008
  • The prevalence extent of Complementary and Alternative Medicine (CAM) use
           among Saudis

    • Authors: Norah A. Alrowais; Nada A. Alyousefi
      Pages: 306 - 318
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): Norah A. Alrowais, Nada A. Alyousefi
      Introduction: There is worldwide interest in the use of CAM. Studying CAM in Saudi population is important as it will reflect the influence of psychosocial, cultural and religious factors on health beliefs and behaviors. The objective of this study was to present an updated review on the use of CAM practices in Saudi Arabia including commonly used types, common conditions for which it has been used and who uses CAM. Methods: This review used data from national surveys conducted in Saudi Arabia and published between 2000 and 2015. The literature search was performed considering standards adopted such as Moose guidelines for observational studies. Two authors independently reviewed each article. The search yielded 73 articles, and a total of 36 articles were included. Further careful data extraction was carried out by two independents reviewers. Results: Most of the reviewed studies were cross-sectional in design and were published between 2014 and 2015, and mostly in Riyadh region. Substantial difference in the findings for the patterns of CAM use was revealed. The most commonly employed practice was of spiritual type such as prayer and reciting Quran alone or on water. Other types include herbs (8–76%), honey (14–73%) and dietary products (6–82%). Cupping (Alhijamah) was least used (4–45%). Acupuncture was more practiced among professionals. Conclusion: The utilization of CAM is widely practiced in Saudi Arabia. There is need for efforts to promote research in the field of CAM to address each practice individually. Population surveys should be encouraged supported by mass media to raise knowledge and awareness about the practice of different CAM modalities. The national center of CAM should play a major role in these efforts.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.09.009
  • Biochemical and molecular modulation of CCl4-induced peripheral and
           central damage by Tilia americana var. mexicana extracts

    • Authors: Elvia Coballase-Urrutia; Noemí Cárdenas-Rodríguez; María Carolina González-García; Eithan Núñez-Ramírez; Esaú Floriano-Sánchez; María Eva González-Trujano; Berenice Fernández-Rojas; José Pedraza-Chaverrí; Hortencia Montesinos-Correa; Liliana Rivera-Espinosa; Aristides III Sampieri; Liliana Carmona-Aparicio
      Pages: 319 - 331
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): Elvia Coballase-Urrutia, Noemí Cárdenas-Rodríguez, María Carolina González-García, Eithan Núñez-Ramírez, Esaú Floriano-Sánchez, María Eva González-Trujano, Berenice Fernández-Rojas, José Pedraza-Chaverrí, Hortencia Montesinos-Correa, Liliana Rivera-Espinosa, Aristides III Sampieri, Liliana Carmona-Aparicio
      Around the world, species from the genus Tilia are commonly used because of their peripheral and central medicinal effects; they are prepared as teas and used as tranquilizing, anticonvulsant, and analgesic agents. In this study, we provide evidence of the protective effects of organic and aqueous extracts (100mg/kg, i.p.) obtained from the leaves of Tilia americana var. mexicana on CCl4-induced liver and brain damage in the rat. Protection was observed in the liver and brain (cerebellum, cortex and cerebral hemispheres) by measuring the activity of antioxidant enzymes and levels of malondialdehyde (MDA) using spectrophotometric methods. Biochemical parameters were also assessed in serum samples from the CCl4-treated rats. The T. americana var. mexicana leaf extracts provided significant protection against CCl4-induced peripheral and central damage by increasing the activity of antioxidant enzymes, diminishing lipid peroxidation, and preventing alterations in biochemical serum parameters, such as the levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), γ-globulin (γ-GLOB), serum albumin (ALB), total bilirubin (BB), creatinine (CREA) and creatine kinase (CK), relative to the control group. Additionally, we correlated gene expression with antioxidant activity in the experimental groups treated with the organic and aqueous Tilia extracts and observed a non-statistically significant positive correlation. Our results provide evidence of the underlying biomedical properties of T. americana var. mexicana that confer its neuro- and hepatoprotective effects.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.06.008
  • Antibiotic prophylaxis in organophosphorus poisoning: A study of health
           and economic outcomes

    • Authors: Asim Priyendu; K.E. Vandana; Nilima; Muralidhar Varma; Nishitha Prabhu; Alsha Abdul Rahim; Anantha Naik Nagappa
      Pages: 332 - 336
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): Asim Priyendu, K.E. Vandana, Nilima, Muralidhar Varma, Nishitha Prabhu, Alsha Abdul Rahim, Anantha Naik Nagappa
      Objective: Organophosphorus poisoning (OPP) is a major concern for developing countries. There are no guidelines for the prophylactic use of antibiotics in the management of OPP which in such critical cases might add to the economic burden of the patients as well as antibiotic resistance. We compared the health and economic outcomes in patients prescribed with prophylactic antibiotics with respect to the patients not prescribed with any antibiotics. Methods: A retrospective observational study was carried out for two years for patients admitted to ICU with OPP. Patients were graded for severity of OPP, and divided into two groups based on prophylactic prescription and no prescription of antibiotics. The length of stay (LOS), hospitalization cost and outcomes were measured and compared between the two groups using statistical tests. Results: Out of the 254 patients observed, 108 were prescribed with prophylactic antibiotics and 94 were not prescribed with any antibiotic. There was a significant difference between LOS, cost of treatment and outcomes in the two groups (p <0.001). When antibiotics were not prescribed, the odds of improvement was 1.854 times higher compared to those who received prophylactic antibiotics although after adjusting for severity of poisoning, significance was lost. On an average, 2–3 antibiotics were prescribed to every patient in the first group. Conclusion: OPP is an important health concern where issues of antibiotic misuse and overuse are practiced. Our study suggested that systemic antibiotic prophylaxis did not offer any advantage over non-use of any antibiotics in patients with OPP.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.07.006
  • Synthesis, characterization and biological evaluation of novel 2,5
           substituted-1,3,4 oxadiazole derivatives

    • Authors: Selvaraj Kavitha; Kulanthai Kannan; Sadhasivam Gnanavel
      Pages: 337 - 345
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): Selvaraj Kavitha, Kulanthai Kannan, Sadhasivam Gnanavel
      In the present study, a series of 3-(5-cyclohexyl-1,3,4-oxadiazol-2-yl)-N-substituted aniline have been synthesized by multistep reaction scheme. Benzohydrazide was used as the starting material. The structures of all synthesized compounds are characterized and confirmed by FT-IR, 1H and C13 NMR and mass spectral studies with the intention of developing the novel biologically active compounds. All title synthetic compounds were screened for their antidiabetic, anti-inflammatory and anticancer activities.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.07.004
  • Direct and enhanced delivery of nanoliposomes of anti schizophrenic agent
           to the brain through nasal route

    • Authors: Pratik Upadhyay; Jatin Trivedi; Kilambi Pundarikakshudu; Navin Sheth
      Pages: 346 - 358
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): Pratik Upadhyay, Jatin Trivedi, Kilambi Pundarikakshudu, Navin Sheth
      The problem of inadequate oral bioavailability of Quetiapine Fumarate, a lipophilic drug used for schizophrenia, due to hepatic metabolism and repulsion by brain barrier was attempted in this study. Combination of two approaches, viz. Quetiapine inclusion into the liposomal carrier for better diffusion and administration through nasal route to avoid hepatic metabolism and barrier elimination was applied. Thin film hydration followed by sonication method was employed in liposome preparation and the formulation was optimized using 32 full factorial design. The number of sonication cycles (X 1) of 2min and 80% amplitude and molar ratio of constructional components such as cholesterol to egg phosphatidylcholine (X 2) as independent variables and a % of entrapment efficiency (Y 1) and cumulative in vitro drug release (Y 2) at 6h as dependent variables was selected. Batch F7 prepared by 2 cycles of sonication and 1:3M ratio of cholesterol:egg phosphatidylcholine was optimized as a consequence of substantial entrapment efficiency of 75.63±3.77%, and 99.92±1.88% drug release and 32.33±1.53% drug diffusion, which was optimum among all other batches at 6h. Diffusion study was done for all the batches of liposomal formulation by using sheep nasal mucosa and good amount with better diffusion rate was measured which proved liposomal dispersion a virtuous delivery system for brain drug delivery through nasal route. Results of in vivo, ciliotoxicity and gamma scintigraphy studies on mice supported the above inference.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.07.003
  • Utilization of gel electrophoreses for the quantitative estimation of
           digestive enzyme papain

    • Authors: Magdy M. Muharram; Maged S. Abdel-Kader
      Pages: 359 - 364
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): Magdy M. Muharram, Maged S. Abdel-Kader
      SDS-PAGE densitometric method for analysis of papain in pharmaceutical formulations was developed and validated for the first time. Standard and samples were mixed with SDS sample buffer and denatured at 95°C for 5min and the gel was run at 20mA and 200V for 30–40min in SDS-PAGE buffer. Gels were stained in Coomassie blue solution and distained by 5% methanol and 10% acetic acid. Destained gels were imaged and analyzed using the ChemiDoc™ XRS+ System. Bands of papain appeared at Rf value 0.78±0.03 corresponding to molecular weight 23406Da between proteins with molecular weight 31,000and21,500Daof the broad range protein standard. The generated calibration curve was used for quantitative estimation of papain in pharmaceutical formulations. The developed method was validated for precision, accuracy, specificity and robustness as described by the ICH guidelines. The proposed method gives an alternative approach for enzymes and protein analysis.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.09.002
  • Comparison of physicochemical properties of suppositories containing
           starch hydrolysates

    • Authors: Piotr Belniak; Katarzyna Świąder; Michał Szumiło; Aleksandra Hyla; Ewa Poleszak
      Pages: 365 - 369
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): Piotr Belniak, Katarzyna Świąder, Michał Szumiło, Aleksandra Hyla, Ewa Poleszak
      The purpose of this work was to determine the effect of starch hydrolysates (SH) on the physicochemical properties of suppositories. The study was conducted with suppositories with acetaminophen (AAP) a typical antipyretic analgesic, as model drug on lipophilic (cocoa butter) and hydrophilic base (polyethylene glycol 1500+400). The suppositories with and without the addition of SH were examined for physicochemical tests according to European Pharmacopoeia 8th edition (Ph. Eur.): the uniformity of mass of single-dose preparation test, the softening time determination of lipophilic suppositories test, the disintegration of suppositories test, and dissolution test with flow-through apparatus. The results confirm the possibility of using starch hydrolysates as a cheap and safe addition to modify physicochemical properties of suppositories.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.09.004
  • Effect of Aster tataricus on production of inflammatory mediators in LPS
           stimulated rat astrocytoma cell line (C6) and THP-1 cells

    • Authors: Hong-tao Zhang; Miao Tian; Qiao-wei He; Nan Chi; Chun-ming Xiu; Yun-bo Wang
      Pages: 370 - 375
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): Hong-tao Zhang, Miao Tian, Qiao-wei He, Nan Chi, Chun-ming Xiu, Yun-bo Wang
      Neuroinflammation is the commonest cause of neurodegenerative diseases such as Alzheimer’s disease. Present investigation evaluates the inhibitory effect of ethanolic root extract of Aster tataricus (AS) on inflammatory mediators production in lipopolysaccharide (LPS) stimulated C6 cells. C6 cells were treated with AS (20and40mg/kg) and nimesulide (NSL, 1.5μg/ml) for 1day. Thereafter various parameters such as production of ROS, release of nitrite, MDA, glutathione level and NF-κB translocation were estimated in C6 cell lines. Effect of AS was estimated on the expressions of tumor necrosis factor α (TNF-α) of human monocytic leukemia cell line (THP-1). It was observed that AS (20and40mg/ml) treated group shows significant (p <0.01) decrease in production of ROS, Nitrite release and MDA level in LPS activated C6 cell lines compared to negative control group. Moreover, treatment with it decreases glutathione level and inhibits the translocation of NF-κB in LPS activated C6 cell lines compared to negative control group. There were significant (p <0.01) decreases in expression of TNF-α in AS treated group compared to negative control group in THP-1 cell lines. Present investigation concludes the anti neuroinflammatory effect of ethanolic extract of AS root by decreasing oxidative stress and attenuates the cytokine.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.09.001
  • CYP2C9, CYPC19 and CYP2D6 gene profiles and gene susceptibility to drug
           response and toxicity in Turkish population

    • Authors: Merve Arici; Gül Özhan
      Pages: 376 - 380
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): Merve Arici, Gül Özhan
      Pharmacogenetics is a vast field covering drug discovery research, the genetic basis of pharmacokinetics and dynamics, genetic testing and clinical management in diseases. Pharmacogenetic approach usually focuses on variations of drug transporters, drug targets, drug metabolizing enzymes and other biomarker genes. Cytochrome P450 (CYP) enzymes, an essential source of variability in drug-response, play role in not only phase I-dependent metabolism of xenobiotics but also metabolism of endogenous compounds such as steroids, vitamins and fatty acids. CYP2C9, CYP2C19 and CYP2D6 enzymes being highly polymorphic are responsible for metabolism of a variety of drug groups. In the study, it was determined the genotype and allele frequency of CYP2C9∗2, CYP2C19∗3, CYP2C19∗2, CYP2C19∗3, CYP2C19∗17, CYP2D6∗9 and CYP2D6∗41, very common and functional single-nucleotide polymorphisms (SNPs), in healthy volunteers. The genotype distributions were consistent with the Hardy-Weinberg equilibrium in the population (p >0.05). It is believed that the determination of polymorphisms in the enzymes may be beneficial in order to prevention or reduction in adverse effects and death. The recessive allele frequencies of CYP2C9∗2, CYP2C19∗3, CYP2C19∗2, CYP2C19∗3, CYP2C19∗17, CYP2D6∗9 and CYP2D6∗41 were 11, 13, 12, 13, 25, 4 and 15%, respectively. According to the obtained results, the carriers of CYP2D6∗9 variant allele should be received higher doses of the drugs metabolizing with this enzyme in Turkish population, while the carriers of other variant alleles do not generally have any requirement of dose regimen.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.09.003
  • Volatile constituents and biological activities of the leaf and root of
           Echinacea species from South Africa

    • Authors: M. Nyalambisa; I.A. Oyemitan; R. Matewu; O.O. Oyedeji; O.S. Oluwafemi; S.P. Songca; B.N. Nkeh-Chungag; A.O. Oyedeji
      Pages: 381 - 386
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): M. Nyalambisa, I.A. Oyemitan, R. Matewu, O.O. Oyedeji, O.S. Oluwafemi, S.P. Songca, B.N. Nkeh-Chungag, A.O. Oyedeji
      Echinacea is used ethnomedicinally for the treatment of various diseases such as cough, respiratory infections, and bronchitis among other uses in Eastern Cape region of South Africa. This study evaluated the volatile components of the essential oil of the plant, its toxicity, anti-inflammatory and analgesic activities in rodents. Dried leaf and root of the plant were separately processed by hydrodistillation for 4 h and their essential oils (EOs) were collected. Extracted oils were subjected to GC/GC–MS analysis. The essential oil was further evaluated for acute toxicity, anti-inflammatory and analgesic activities. The toxicity profile of the essential oil was evaluated in mice through the oral route (p.o.), and anti-inflammatory activity was evaluated on the carrageenan-induced edema model in rats at the doses of 100–200mg/kg, while its analgesic effect was evaluated on the acetic acid-induced writhings model in mice at doses of 100–200mg/kg. GC/GC–MS analysis of EOs showed that a number of compounds identified in the leaf and root oils were 25 and 31 respectively. The chemical compositions of the oils varied and the major compounds identified in the oils include germacrene D, naphthalene, caryophyllene oxide, α-phellandrene and α-cadinol. The essential root oil did not cause mortality at the highest dose of 5000mg/kg; hence, its LD50 was estimated to be ⩾5000mg/kg, p.o. The anti-inflammatory test results showed that the essential root oil caused significant (p <0.05–0.01) reduction in edema size compared to the negative control group on the carrageenan-induced edema and the results for the analgesic test showed that the essential root oil caused significant (p <0.05) reduction in number of writhings at 1000mg/kg compared to the negative control group. It is concluded that root and leaf of this Echinacea species contain volatile oils which varied in their yield and chemical compositions. The essential root oil is non-toxic orally and it demonstrated significant anti-inflammatory and analgesic activities in laboratory animals.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.09.010
  • Prophylactic and curative anti-ulcerogenic activity and the possible
           mechanisms of action of some desert plants

    • Authors: Reham M. El-Meligy; Amani S. Awaad; Gamal A. Soliman; Sanaa A. Kenawy; Saleh I. Alqasoumi
      Pages: 387 - 396
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): Reham M. El-Meligy, Amani S. Awaad, Gamal A. Soliman, Sanaa A. Kenawy, Saleh I. Alqasoumi
      The present study aimed to evaluate the anti-ulcerogenic activities and the possible mechanisms of action of seven desert plants from different families. Conyza dioscoridis (L.) Desf. (Asteraceae), Euphorbia hirta L. (Euphorpiaceae), Origanum syriacum L., Salvia lanigera L. (Lamiaceae), Sisymbrium irio L., Solanum nigrum Linn. (Solanaceae) and Solenostemma arghel (Del.) Hayne. (Asclepiadaceae), were tested using prophylactic and curative models of absolute ethanol-induced ulcer, at three doses (125, 250 & 500mg/kg) of each extract. The investigated extracts possessed dose dependent anti-ulcerogenic activities in both models, with LD50 higher than 5g/kg. The most effective extracts were C. dioscoridis and S. irio with percent protection of control ulcer; 91.1% and 85.4% respectively. The antisecretory activity of both C. dioscoridis and S. irio appears to be mainly related to the suppression of gastrin release. The in vitro potential radical (DPPH) scavenging activities of the investigated extracts were well supported with the reduction in gastric MDA (50.6% and 43.3%) and enhancing the level of reduced GSH (2.84, 2.59mg/g tissue) for C. dioscoridis and S. irio respectively. In addition, suppression of the inflammatory mediator TNF-α may be one of the possible mechanisms of action. The alcohol extracts of C. dioscoridis and S. irio showed no alteration on liver and kidney functions. Phytochemical screening of the investigated extracts revealed the presence of flavonoids, tannins and sterols which could be related to the activities.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.10.008
  • Enantioselective analysis of fluoxetine in pharmaceutical formulations by
           capillary zone electrophoresis

    • Authors: Melania Cârcu-Dobrin; Monica Budău; Gabriel Hancu; Laszlo Gagyi; Aura Rusu; Hajnal Kelemen
      Pages: 397 - 403
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): Melania Cârcu-Dobrin, Monica Budău, Gabriel Hancu, Laszlo Gagyi, Aura Rusu, Hajnal Kelemen
      Fluoxetine is an antidepressant, a selective serotonin reuptake inhibitor (SSRI) used primarily in the treatment of major depression, panic disorder and obsessive compulsive disorder. Chiral separation of racemic fluoxetine is necessary due to its enantioselective metabolism. In order to develop a suitable method for chiral separation of fluoxetine, cyclodextrin (CD) modified capillary electrophoresis (CE) was employed. A large number of native and derivatized, neutral and ionized CD derivatives were screened to find the optimal chiral selector. As a result of this process, heptakis(2,3,6-tri-O-methyl)-β-CD (TRIMEB) was selected for enantiomeric discrimination. A factorial analysis study was performed by orthogonal experimental design in which several factors are varied at the same time to optimize the separation method. The optimized method (50mMphosphate buffer, pH=5.0, 10mMTRIMEB, 15°C, + 20kV, 50mbar/1s, detection at 230nm) was successful for baseline separation of fluoxetine enantiomers within 5min. Our method was validated according to ICH guidelines and proved to be sensitive, linear, accurate and precise for the chiral separation of fluoxetine.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.09.007
  • The impact of formulation attributes and process parameters on black seed
           oil loaded liposomes and their performance in animal models of analgesia

    • Authors: Zerin T. Rushmi; Nasrin Akter; Rabeya J. Mow; Merina Afroz; Mohsin Kazi; Marcel de Matas; Mahbubur Rahman; Mohammad H. Shariare
      Pages: 404 - 412
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): Zerin T. Rushmi, Nasrin Akter, Rabeya J. Mow, Merina Afroz, Mohsin Kazi, Marcel de Matas, Mahbubur Rahman, Mohammad H. Shariare
      This study aimed to formulate black seed oil (Nigella sativa) loaded liposomes using the ethanol injection method to enhance oral bioavailability and improve therapeutic activity in small animal studies of analgesia. The impact of formulation attributes and process parameters on the liposomal system was evaluated with key quality attributes being particle size, morphology, and entrapment efficiency. The particle size and entrapment efficiency of the liposome preparation were found to be between the range of 50–900nm and 34–87% respectively. Particle size distribution data suggested that increasing the percentage of oil, up to a certain concentration, reduced the size of the liposomes significantly from 520±81.2nm to 51.48±1.31nm. Stirring and injection rate were shown to have marked impact on the average particle size of liposome. It was observed that entrapment efficiency of liposomes was greatly influenced by the amount of cholesterol and type of cryoprotectant used during formulation. The stability study indicated that the liposomal preparation was stable at ambient conditions for one month. In vivo studies showed that the liposomal preparation demonstrated significant analgesic activity in mice.
      Graphical abstract image

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.09.011
  • Effect of nitazoxanide on albendazole pharmacokinetics in cerebrospinal
           fluid and plasma in rats

    • Authors: María Isabel Ruiz-Olmedo; Iliana González-Hernández; Francisca Palomares-Alonso; Javier Franco-Pérez; María de Lourdes González F.; Helgi Jung-Cook
      Pages: 413 - 418
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): María Isabel Ruiz-Olmedo, Iliana González-Hernández, Francisca Palomares-Alonso, Javier Franco-Pérez, María de Lourdes González F., Helgi Jung-Cook
      Background: Although albendazole is the drug-of-choice for the treatment of neurocysticercosis, its efficacy is limited due to its low bioavailability. An alternative for optimizing pharmacological treatment is through drug combinations. In vitro studies have shown that nitazoxanide and tizoxanide (the active metabolite of nitazoxanide) exhibit cysticidal activity and that the combination of tizoxanide with albendazole sulfoxide (the active metabolite of albendazole) produced an additive effect. Objectives: (1) To assess the concentration profile of tizoxanide in plasma and in cerebrospinal fluid; and (2) to evaluate the influence of nitazoxanide on the pharmacokinetics of albendazole in plasma and in cerebrospinal fluid. Methods: Two different studies were conducted. In study 1, 10 male Sprague-Dawley rats received a single oral dose of 7.5mg/kg of nitazoxanide and serial blood and cerebrospinal fluid samples were collected over a period of 4h. In study 2, 38 healthy male Sprague-Dawley rats were randomly divided into two groups: one of these received a single dose of albendazole (15mg/kg) and, in the other group, albendazole (15mg/kg) was co-administered with nitazoxanide (7.5mg/kg). Plasma and cerebrospinal fluid samples were collected from 0 to 16h after administration. Albendazole sulfoxide and tizoxanide levels were assayed by using HPLC or LC/MS techniques. Results: In study 1, tizoxanide reached a maximum plasma concentration of 244.42±31.98ng/mL at 0.25h; however, in cerebrospinal fluid, this could be detected only at 0.5h, and levels were below the quantification limit (10ng/mL). These data indicate low permeation of tizoxanide into the blood brain barrier. In study 2, Cmax, the area under the curve, and the mean residence time of albendazole sulfoxide in plasma and cerebrospinal fluid were not affected by co-administration with nitazoxanide. Conclusion: The results of the present study indicate that in rats at the applied doses, tizoxanide does not permeate into the cerebrospinal fluid. Furthermore, nitazoxanide does not appear to alter significantly the pharmacokinetics of albendazole in plasma or in cerebrospinal fluid.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.09.005
  • Investigation of the in vitro performance difference of drug-Soluplus®
           and drug-PEG 6000 dispersions when prepared using spray drying or

    • Authors: Mohammad A. Altamimi; Steven H. Neau
      Pages: 419 - 439
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): Mohammad A. Altamimi, Steven H. Neau
      Purpose: To evaluate the physicochemical and in vitro characteristics of solid dispersions using BCS II model drugs with Soluplus® and one of its component homopolymers, PEG 6000. Methods: Nifedipine (NIF) and sulfamethoxazole (SMX) of 99.3% and 99.5% purity, respectively, were selected as BCS II model drugs, such that an improved dissolution rate and concentration in the gastrointestinal tract should increase oral bioavailability. Soluplus® is an amorphous, tri-block, graft co-polymer with polyvinyl caprolactam, polyvinyl acetate, and polyethylene glycol (PCL:PVAc:PEG6000) in the ratio 57:30:13. PEG 6000 (BASF) is a waxy material with melting point of about 60°C. Solid dispersions were prepared using lyophilization or spray drying techniques. Dissolution study, crystallinity content, and analysis for new chemical bond formation have been used to evaluate the dispersed materials. Results: Although each polymer improved the drug dissolution rate, dissolution from Soluplus® was slower. Enhanced dissolution rates were observed with NIF solid dispersions, but the dissolution profiles were quite different due to the selected technique, polymer, and dissolution medium. For SMX, there was similarity across the dissolution profiles despite the medium, polymer, or applied technique. Each polymer was able to maintain an elevated drug concentration over the three hour duration of the dissolution profile, i.e., supersaturation was supported by the polymer. DSC thermograms revealed no melting endotherm, suggesting that the drug is amorphous or molecularly dispersed. Conclusion: NIF and SMX solid dispersions were successfully prepared by spray drying and lyophilization using Soluplus® or PEG 6000. Each polymer enhanced the drug dissolution rate; NIF dissolution rate was improved to a greater extent. Dispersions with PEG 6000 had a faster dissolution rate due to its hydrophilic nature. DSC analysis showed that no crystalline material exists in the dispersions.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.09.013
  • New microbial source of the antifungal allylamine

    • Authors: Maged S. Abdel-Kader; Magdy M. Muharram
      Pages: 440 - 442
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): Maged S. Abdel-Kader, Magdy M. Muharram
      The isolated active compound “F12” from the culture media of the Streptomyces sp. KH-F12 was identified using different spectroscopic techniques. Both 1D- and 2D-NMR as well as HRESIMS were utilized to characterize the structure of the isolated compound. ‘F12” was found to be the known systemic antifungal drug terbinafine marketed under the name “Lamisil”. Full analysis of the COSY, HSQC and HMBC enables the full assignment of proton and carbon atoms. Terbinafine is a synthetic allylamine and is reported here for the first time from natural source.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.06.006
  • Plant growth and diosgenin enhancement effect of silver nanoparticles in
           Fenugreek (Trigonella foenum-graecum L.)

    • Authors: B. Jasim; Roshmi Thomas; Jyothis Mathew; E.K. Radhakrishnan
      Pages: 443 - 447
      Abstract: Publication date: March 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 3
      Author(s): B. Jasim, Roshmi Thomas, Jyothis Mathew, E.K. Radhakrishnan
      Various methods have been used to enhance production of chemically diverse phytochemicals especially medicinal natural products. With the advancement in nanotechnology, nanoparticles have been reported to have varying impact in plant growth and inducibility of phytochemical composition. Major objective of the study was to study the secondary metabolite modulatory effect of silver nanoparticles. In the current study, treatment of fenugreek seedlings with biosynthesized silver nanoparticles (Ag-NPs) was found to have significant impact on its growth parameters such as leaf number, root length, shoot length and wet weight. On HPLC based analysis, Ag-NPs treated seedlings showed an enhancement in the production of major phytochemical diosgenin to a level of 214.06±17.07μg/mL. An untreated control gave an yield of only 164.44±7.67μg/mL of diosgenin, and the observed phytochemical enhancement effect induced by Ag-NP was very significant. Most remarkably, the Ag-NP used in the study was found to play dual role of enhancement of both plant growth and diosgenin synthesis. Hence the study is of immense application as it opens up development of new methods based on nanoelicitors to enhance the biosynthesis of medicinal natural products in plants.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2016.09.012
  • The Pharmacological Potential of Rutin

    • Authors: Aditya Ganeshpurkar; Ajay K. Saluja
      Pages: 149 - 164
      Abstract: Publication date: February 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 2
      Author(s): Aditya Ganeshpurkar, Ajay K. Saluja
      The contemporary scientific community has presently recognized flavonoids to be a unique class of therapeutic molecules due to their diverse therapeutic properties. Of these, rutin, also known as vitamin P or rutoside, has been explored for a number of pharmacological effects. Tea leaves, apples, and many more possess rutin as one of the active constituents. Today, rutin has been observed for its nutraceutical effect. The present review highlights current information and health-promoting effects of rutin. Along with this, safety pharmacology issues and SAR of the same have also been discussed.

      PubDate: 2017-03-16T15:11:35Z
      DOI: 10.1016/j.jsps.2016.04.025
  • An overview of pharmacodynamic modelling, ligand-binding approach and its
           application in clinical practice

    • Authors: Mohammed Saji Salahudeen; Prasad S. Nishtala
      Pages: 165 - 175
      Abstract: Publication date: February 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 2
      Author(s): Mohammed Saji Salahudeen, Prasad S. Nishtala
      The study of the magnitude and variation of drug response is defined as pharmacodynamics (PDs). PD models examine plasma concentration and effect relationship. It can predict the archetypal effect ( E ) of a drug as a function of the drug concentration ( C ) and estimate an unknown PD parameter ( θ pd ). The PD models have been described as fixed, linear, log-linear, E max , sigmoid E max , and indirect PD response. Ligand binding model is an example of a PD model that works on the underpinning PD principle of a drug, eliciting its pharmacological effect at the receptor site. The pharmacological effect is produced by the drug binding to the receptor to either activate or antagonise the receptor. Ligand binding models describe a system of interacting components, i.e. the interaction of one or more ligands with one or more binding sites. The E max model is the central method that provides an empirical justification for the concentration/dose-effect relationship. However, for ligand binding models justification is provided by theory of receptor occupancy. In essence, for ligand binding models, the term fractional occupancy is best used to describe the fraction of receptors occupied at a particular ligand concentration. It is stated that the fractional occupancy = occupied binding sites / total binding sites , which means the effect of a drug should depend on the fraction of receptors that are occupied. In the future, network-based systems pharmacology models using ligand binding principles could be an effective way of understanding drug-related adverse effects. This will facilitate and strengthen the development of rational drug therapy in clinical practice.

      PubDate: 2017-03-16T15:11:35Z
      DOI: 10.1016/j.jsps.2016.07.002
  • Temperature excursion management: A novel approach of quality system in
           pharmaceutical industry

    • Authors: Nirmal Kumar; Ajeya Jha
      Pages: 176 - 183
      Abstract: Publication date: February 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 2
      Author(s): Nirmal Kumar, Ajeya Jha
      Quality of pharmaceutical product largely depends upon the environment controls during its storage and handling. Each pharmaceutical product should be handled and stored under specified storage condition labelled on product information data sheet or product pack. Hence the temperature excursions during receipt of raw materials, manufacturing of pharmaceutical products and distribution should be managed during entire product life cycle with holistic approach. The research is based on primary data and exploratory study through literature review. The temperature excursion may be observed during transportation of raw materials manufacturing as well as distribution of pharmaceutical products, which have potential to deteriorate the product quality. Temperature excursion in pharmaceutical industry should be recorded and reported to the manufacturer for further investigation and risk analysis. The concept of temperature excursions, its reasons, consequences and handling mechanism should be well understood to ensure the concerted efforts under the aegis of Quality Management System. Based on the reasons and consequences of temperature excursions during pharmaceutical operations, a system based quality management has been envisaged through this study. The concept and procedure to handle temperature excursion have evolved after this study which shall be useful to pharmaceutical industry as well as to medicine distributors and consumers.

      PubDate: 2017-03-16T15:11:35Z
      DOI: 10.1016/j.jsps.2016.07.001
  • High-performance thin layer chromatography based assay and stress study of
           a rare steroidal alkaloid solanopubamine in six species of Solanum grown
           in Saudi Arabia

    • Authors: Nasir A. Siddiqui; Mohammad K. Parvez; Adnan J. Al-Rehaily; Mohammed S. Al Dosari; Perwez Alam; Faiyaz Shakeel; Hattan A. Al Harbi
      Pages: 184 - 195
      Abstract: Publication date: February 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 2
      Author(s): Nasir A. Siddiqui, Mohammad K. Parvez, Adnan J. Al-Rehaily, Mohammed S. Al Dosari, Perwez Alam, Faiyaz Shakeel, Hattan A. Al Harbi
      The present study describes a method developed for quantification and stability study of a rare steroidal alkaloid solanopubamine (SPN) in aerial parts of six different species of genus Solanum extracted with two different solvents. The Solanum species selected for investigation include S. schimperianum (SS), S. villosum (SV), S. coagulans (SC), S. glabratum (SG), S. incanum (SI) and S. nigrum (SN). The estimation of SPN was done by a validated high-performance thin layer chromatography method. The developed chromatographic system was found to give a sharp spot for solanopubamine at Rf =0.39±0.01. The steroidal alkaloid SPN was observed to be present only in extracts of aerial parts of S. schimperianum. The sensitivity of developed method produced 40ng and 115ngband−1, respectively as LOD and LOQ values. The percentage yield of SPN in aerial parts of S. schimperianum extracted by ethanol (95%) only and a mixture of ethanol and ammonium hydroxide (6:4) was found to be 1.03w/w and 2.09w/w, respectively. Stability studies of SPN exhibited the maximum (100%) degradation in an alkaline environment and H2O2 treated samples and 61.4% in acidic conditions. The SPN was found to be significantly stable against UV exposure, photo-oxidation and at room temperature while 13.83% and 57.88% destruction has been observed when exposed to dry heat at 40°C and 60°C, respectively.

      PubDate: 2017-03-16T15:11:35Z
      DOI: 10.1016/j.jsps.2016.05.003
  • Acute toxicity profiling of the ethyl acetate fraction of Swietenia
           macrophylla seeds and in-vitro neuroprotection studies

    • Authors: Mustak Sayyad; Ning Tiang; Yatinesh Kumari; Bey Hing Goh; Yogini Jaiswal; Rozita Rosli; Leonard Williams; Mohd Farooq Shaikh
      Pages: 196 - 205
      Abstract: Publication date: February 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 2
      Author(s): Mustak Sayyad, Ning Tiang, Yatinesh Kumari, Bey Hing Goh, Yogini Jaiswal, Rozita Rosli, Leonard Williams, Mohd Farooq Shaikh
      Swietenia macrophylla (SM) is a medicinally important plant found in tropical and subtropical regions of the world. The ethyl acetate fraction of the seeds of S. macrophylla (SMEAF) is reported to exhibit potent anticancer, antitumor, anti-inflammatory and antifeedant activities. Till date, there have been no studies reported on the acute oral toxicity profile of the ethyl acetate fraction of the seeds of SM. The objective of the present study was to determine the acute toxicity of SMEAF and evaluate the in-vitro neuroprotective activity of SMEAF using primary neuronal cell cultures. In acute oral toxicity study, the SMEAF did not produce any lethal signs of morbidity and mortality. Histo-pathological findings, support the safety of SMEAF, as there were no significant changes observed in any of the parameters studied. Based on the results obtained in MTT assay, we infer that SMEAF has a significant neuroprotective effect, as it increased the cell viability and exhibited protection to the neuronal cells against TBHP induced oxidative stress. Thus, SMEAF can be suggested for use in the development of herbal drug formulations with neuroprotective potential.

      PubDate: 2017-03-16T15:11:35Z
      DOI: 10.1016/j.jsps.2016.05.002
  • Prolonged exposure of colon cancer cells to 5-fluorouracil nanoparticles
           improves its anticancer activity

    • Authors: Essam Tawfik; Maqusood Ahamed; Abdulaziz Almalik; Mohammad Alfaqeeh; Aws Alshamsan
      Pages: 206 - 213
      Abstract: Publication date: February 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 2
      Author(s): Essam Tawfik, Maqusood Ahamed, Abdulaziz Almalik, Mohammad Alfaqeeh, Aws Alshamsan
      In this study, we aimed to improve the anticancer effect of 5-FU on human colon cancer cell lines by incorporating in poly(d,l lactic-co-glycolic acid) (PLGA) nanoparticles (NPs). The 5-FU-PLGA NPs were prepared by nanoprecipitation technique. Prepared NPs were moderately dispersed with an average diameter of 133±25.19nm. Scanning Electron Microscope (SEM) images revealed spherical structures with subtle surface irregularity. Free 5-FU dose–response curves were constructed (12.5–2000μM) using MTT assay on HCT 116 and HT-29 cell lines for 1, 3, and 5days. The calculated IC50 on HCT 116 were 185μM after 1day, 11.3μM after 3days, and 1.48μM after 5days. On HT-29, IC50 was only reached after 5days of 5-FU treatment (11.25μM). The HCT 116 viability following treatment with 100μM 5-FU in free or NPs forms for 3days was 38.8% and 18.6%, respectively. Similarly, when 250μM was applied, HCT 116 viability was 17.03% and 14.6% after treatment with free and NPs forms of 5-FU, respectively. Moreover, HT-29 cell viability after 250μM 5-FU treatment in free or NPs forms was 55.45% and 34.01%, respectively. We also noticed that HCT 116 cells were more sensitive to 5-FU-PLGA NPs as compared to HT-29 cells. Overall, our data indicate that 5-FU activity is time dependent and the prolonged effects created by PLGA NPs may contribute, at least in part, to the noticed enhancement of the anticancer activity of 5-FU drug.

      PubDate: 2017-03-16T15:11:35Z
      DOI: 10.1016/j.jsps.2016.05.010
  • Synthesis and evaluation of anticancer activity of 6-pyrazolinylcoumarin

    • Authors: Yana Garazd; Myroslav Garazd; Roman Lesyk
      Pages: 214 - 223
      Abstract: Publication date: February 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 2
      Author(s): Yana Garazd, Myroslav Garazd, Roman Lesyk
      A series of novel 6-pyrazolinylcoumarins has been synthesized via multi-step protocol. The synthetic procedure was based on the acetylation of hydroxycoumarins; Fries rearrangement and Claisen–Schmidt condensation; the target 6-[5-aryl-4,5-dihydropyrazol-3-yl]-5-hydroxy-7-methylcoumarins (33–49) were obtained under reactions of hydrazine and 2-aryl-5-methyl-2,3-dihydropyrano[2,3-f]chromen-4,8-diones as the last phase of the protocol. Anticancer activity screening in NCI60-cell lines assay allowed identification of compound 47 with the highest level of antimitotic activity with mean GI50 value of 10.20μM and certain sensitivity profile toward the Leukemia cell lines CCRF-CEM and MOLT-4 (GI50/TGI values 1.88/5.06μM and 1.92/4.04μM respectively).

      PubDate: 2017-03-16T15:11:35Z
      DOI: 10.1016/j.jsps.2016.05.005
  • Prevalence of UDP-glucuronosyltransferase polymorphisms (UGT1A6∗2,
           1A7∗12, 1A8∗3, 1A9∗3, 2B7∗2, and 2B15∗2) in a Saudi population

    • Authors: Khalid M. Alkharfy; Basit L. Jan; Sibtain Afzal; Fahad I. Al-Jenoobi; Abdullah M. Al-Mohizea; Saleh Al-Muhsen; Rabih Halwani; Mohammad K. Parvez; Mohammed S. Al-Dosari
      Pages: 224 - 230
      Abstract: Publication date: February 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 2
      Author(s): Khalid M. Alkharfy, Basit L. Jan, Sibtain Afzal, Fahad I. Al-Jenoobi, Abdullah M. Al-Mohizea, Saleh Al-Muhsen, Rabih Halwani, Mohammad K. Parvez, Mohammed S. Al-Dosari
      Glucuronidation is an important phase II pathway responsible for many endogenous substances and drug metabolism. The present work evaluated allele frequencies of certain UDP-glucuronosyl-transferases (UGT 1A6∗2, A7∗12, A8∗3, A9∗3, 2B7∗2, and 2B15∗2) in Saudi Arabians that could provide essential ethnic information. Blood samples from 192 healthy unrelated Saudi males of various geographic regions were collected. Genomic DNA was isolated and genotyping of various UGTs was carried out using polymerase chain reaction (PCR) followed by direct sequencing. For UGT1A6∗2 A/G genotype, the most common variant was the homozygous repeat (AA) and the most common allele was (A) with a frequency of 46.5% and 67.3%, respectively. Similarly, the most common variant for UGT1A7∗12 T/C genotype was the heterozygous repeat (TC) with a frequency of 78.7% while the mutant allele (C) was present in 60.6% of the study population. Both UGT1A8∗3 (G/A) and UGT1A9∗3 (T/C) showed only a wild homozygous pattern in all screened subjects. For UGT2B7∗2, the heterozygous repeat (TC) was found with a frequency of 57.3% and the alleles (A) showed a frequency of 50.8%. In contrast, for UGT2B15∗2 (G253T), the heterozygous repeat (TG) presented 62.3% of the subjects where the most common allele (G) was with a frequency of 66.2%. In conclusion, our data indicate that Saudis harbor some important UGT mutations known to affect enzyme activity. Additional studies are therefore, warranted to assess the clinical implications of these gene polymorphisms in this ethnic group.

      PubDate: 2017-03-16T15:11:35Z
      DOI: 10.1016/j.jsps.2016.05.009
  • d-α-tocopherol nanoemulsions: Size properties, rheological behavior,
           surface tension, osmolarity and cytotoxicity

    • Authors: M.C. Teixeira; P. Severino; T. Andreani; P. Boonme; A. Santini; A.M. Silva; E.B. Souto
      Pages: 231 - 235
      Abstract: Publication date: February 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 2
      Author(s): M.C. Teixeira, P. Severino, T. Andreani, P. Boonme, A. Santini, A.M. Silva, E.B. Souto
      The aim of this study was the assessment of the physicochemical stability of d-α-tocopherol formulated in medium chain triglyceride nanoemulsions, stabilized with Tween®80 and Lipoid®S75 as surfactant and co-surfactant, respectively. d-α-tocopherol was selected as active ingredient because of its well-recognized interesting anti-oxidant properties (such as radical scavenger) for food and pharmaceutical industries. A series of nanoemulsions of mean droplet size below 90nm (polydispersity index<0.15) have been produced by high-pressure homogenization, and their surface electrical charge (zeta potential), pH, surface tension, osmolarity, and rheological behavior, were characterized as a function of the d-α-tocopherol loading. In vitro studies in Caco-2 cell lines confirmed the safety profile of the developed nanoemulsions with percentage of cell viability above 90% for all formulations.

      PubDate: 2017-03-16T15:11:35Z
      DOI: 10.1016/j.jsps.2016.06.004
  • Biologically-guided isolation of leishmanicidal secondary metabolites from
           Euphorbia peplus L.

    • Authors: Elham Amin; Abeer Moawad; Hossam Hassan
      Pages: 236 - 240
      Abstract: Publication date: February 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 2
      Author(s): Elham Amin, Abeer Moawad, Hossam Hassan
      Leishmaniasis is a worldwide health problem, highly endemic in developing countries. Moreover, the severe side effects and the reported drug resistance make it an urgent need to search for effective drugs that can replace or supplement those currently used. In a research program designed to investigate the antileishmanial activity of plants collected from the Egyptian flora, twenty extracts from fifteen plants growing in Egypt have been investigated for in vitro leishmanicidal activity against Leishmania donovani promastigotes. Among the tested extracts, the methanol extract of Euphorbia peplus aerial parts exhibited a significant antileishmanial activity as it produced 100% inhibition of growth with activity similar to amphotericin B. The total extract was subjected to liquid-liquid fractionation using solvents of different polarities, followed by testing the antileishmanial activity of the successive fractions. Phytochemical exploration of the active n-hexane fraction (which produced 75% inhibition of growth) led to isolation of four compounds: simiarenol (1), 1-hexacosanol (2), β-sitosterol (3), and β-sitosterol-3-O-glucoside (4) from the biologically active sub-fractions. Structure elucidation was aided by 1D and 2D NMR techniques. In conclusion, E. peplus plant has many non-polar secondary metabolites that can be used as drug leads for treatment of leishmaniasis.

      PubDate: 2017-03-16T15:11:35Z
      DOI: 10.1016/j.jsps.2016.06.003
  • Antiproliferative and apoptotic effect of Morus nigra extract on human
           prostate cancer cells

    • Authors: Ibrahim Turan; Selim Demir; Kagan Kilinc; Nesibe Arslan Burnaz; Serap Ozer Yaman; Kubra Akbulut; Ahmet Mentese; Yuksel Aliyazicioglu; Orhan Deger
      Pages: 241 - 248
      Abstract: Publication date: February 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 2
      Author(s): Ibrahim Turan, Selim Demir, Kagan Kilinc, Nesibe Arslan Burnaz, Serap Ozer Yaman, Kubra Akbulut, Ahmet Mentese, Yuksel Aliyazicioglu, Orhan Deger
      Background: Morus nigra L. belongs to the family Moraceae and is frequently used in traditional medicine. Numerous studies have investigated the antiproliferative effects of various extracts of different Morus species, but studies involving the in vitro cytotoxic effect of M. nigra extract are very limited. The purpose of this study was to evaluate the phenolic composition and antioxidant activity of dimethyl sulfoxide extract of M. nigra (DEM) and to investigate, for the first time, the probable cytotoxic effect in human prostate adenocarcinoma (PC-3) cells together with the mechanism involved. Methods: Total polyphenolic contents (TPC), ferric reducing antioxidant power (FRAP) and phenolic compounds of DEM were evaluated using spectrophotometric procedures and HPLC. The cytotoxic effect of DEM on PC-3 cells was revealed using the MTT assay. Mechanisms involved in the cytotoxic effect of DEM on PC-3 cells were then investigated in terms of apoptosis, mitochondrial membrane potential and cell cycle using flow cytometry, while caspase activity was investigated using luminometric analysis. Results: TPC and FRAP values were 20.7±0.3mg gallic acid equivalents and 48.8±1.6mg trolox equivalents per g sample, respectively. Ascorbic acid and chlorogenic acid were the major phenolic compounds detected at HPLC analysis. DEM arrested the cell cycle of PC-3 cells at the G1 phase, induced apoptosis via increased caspase activity and reduced mitochondrial membrane potential. Conclusions: Our results indicate that M. nigra may be a novel candidate for the development of new natural product based therapeutic agents against prostate cancer.

      PubDate: 2017-03-16T15:11:35Z
      DOI: 10.1016/j.jsps.2016.06.002
  • Effect of Pelargonidin isolated from Ficus benghalensis L. on phenotypic
           changes in zebrafish (Danio rerio) embryos

    • Authors: Uday Kundap; Yogini Jaiswal; Rachana Sarawade; Leonard Williams; Mohd. Farooq Shaikh
      Pages: 249 - 257
      Abstract: Publication date: February 2017
      Source:Saudi Pharmaceutical Journal, Volume 25, Issue 2
      Author(s): Uday Kundap, Yogini Jaiswal, Rachana Sarawade, Leonard Williams, Mohd. Farooq Shaikh
      In the present study, the extraction and isolation of Pelargonidin, an anthocyanin compound from stem bark of Ficus benghalensis are described. The study also involves evaluation of the effect of Pelargonidin on phenotypic variations in zebra fish embryos. Extraction and isolation of Pelargonidin were carried out by employing liquid-liquid extraction technique, phytochemical tests, column chromatography, UV and FT-IR. In the zebra fish embryo model, Paclitaxel was employed as a negative control. A series of phenotypic changes in different stages of embryonic development were studied with treatment concentrations of Pelargonidin between 3.0 and 20ppm at 0–72-hour post-fertilization (hpf). The results of our studies indicate that, after exposure of zebra fish embryos to 3.3–20ppm concentration of Pelargonidin for 72h, a significant reduction in aortic development occurs. At the dose level of 0.5ppm Paclitaxel and Pelargonidin in the dose range between 3.3 and 20ppm, the zebra fish embryos were found to have bent tail, malformed eyes and developmental delays in vasculature. Based on the results obtained, we infer that Pelargonidin can exhibit phenotypic anti-angiogenic variations in embryonic stage of fish embryos and it can be applied in future for exploration of its anti-angiogenic potential. Furthermore, Pelargonidin could serve as a candidate drug for in vivo inhibition of angiogenesis and can be applied for the treatment of neovascular diseases and tumor.

      PubDate: 2017-03-16T15:11:35Z
      DOI: 10.1016/j.jsps.2016.06.010
  • Vapour-phase method in the synthesis of polymer-ibuprofen sodium-silica
           gel composites

    • Authors: Agnieszka Kierys; Patrycja Krasucka; Marta Grochowicz
      Abstract: Publication date: Available online 20 March 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Agnieszka Kierys, Patrycja Krasucka, Marta Grochowicz
      The study discusses the synthesis of polymer-silica composites comprising water soluble drug (ibuprofen sodium, IBS). The polymers selected for this study were poly(TRIM) and poly(HEMA-co-TRIM) produced in the form of permanently porous beads via the suspension-emulsion polymerization method. The acid and base set ternary composites were prepared by the saturation of the solid dispersions of drug (poly(TRIM)-IBS and/or poly(HEMA-co-TRIM)-IBS) with TEOS, and followed by their exposition to the vapour mixture of water and ammonia, or water and hydrochloric acid, at autogenous pressure. The conducted analyses reveal that the internal structure and total porosity of the resulting composites strongly depend on the catalyst which was used for silica precursor gelation. The parameters characterizing the porosity of both of the acid set composites are much lower than the parameters of the base set composites. Moreover, the basic catalyst supplied in the vapour phase does not affect the ibuprofen sodium molecules, whereas the acid one causes transformation of the ibuprofen sodium into the sodium chloride and a derivative of propanoic acid, which is poorly water soluble. The release profiles of ibuprofen sodium from composites demonstrate that there are differences in the rate and efficiency of drug desorption from them. They are mainly affected by the chemical character of the polymeric carrier but are also associated with the restricted swelling of the composites in the buffer solution after precipitation of silica gel.

      PubDate: 2017-03-22T08:29:53Z
      DOI: 10.1016/j.jsps.2017.03.004
  • High resolution UHPLC-MS characterization and isolation of main compounds
           from the antioxidant medicinal plant Parastrephia lucida (Meyen)

    • Authors: Carlos Echiburu-Chau; Leyla Pastén; Claudio Parra; Jorge Bórquez; Andrei Mocan; Mario J. Simirgiotis
      Abstract: Publication date: Available online 14 March 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Carlos Echiburu-Chau, Leyla Pastén, Claudio Parra, Jorge Bórquez, Andrei Mocan, Mario J. Simirgiotis
      High-resolution mass spectrometry is currently used to determine the mass of biologically active compounds in medicinal plants and food and UHPLC-Orbitrap is a relatively new technology that allows fast fingerprinting and metabolomics analysis. Forty two metabolites including several phenolic acids, flavonoids, coumarines, tremetones and ent-clerodane diterpenes were accurately identified for the first time in the resin of the medicinal plant Parastrephia lucida (Asteraceae) a Chilean native species, commonly called Siputola, collected in the pre-cordillera and altiplano regions of northern Chile, by means of UHPLC-PDA-HR-MS. This could be possible by the state of the art technology employed, which allowed well resolved total ion current peaks and the proposal of some biosynthetic relationships between the compounds detected. Some mayor compounds were also isolated using HSCCC. The ethanolic extract showed high total polyphenols content and significant antioxidant capacity. Furthermore, several biological assays were performed that determined the high antioxidant capacity found for the mayor compound isolated from the plant, 11- p-coumaroyloxyltremetone.
      Graphical abstract image

      PubDate: 2017-03-16T15:11:35Z
      DOI: 10.1016/j.jsps.2017.03.001
  • Comparative Study Of Free And Liposome-Entrapped Chloramphenicol Against
           Biofilms Of Potentially Pathogenic Bacteria Isolated From Cooling Towers

    • Authors: Marcus Vinícius Dias-Souza; Daniel Lucas Soares; Vera Lúcia dos Santos
      Abstract: Publication date: Available online 12 March 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Marcus Vinícius Dias-Souza, Daniel Lucas Soares, Vera Lúcia dos Santos
      This study aimed to investigate for the first time the in vitro antibiofilm effectiveness of two chloramphenicol liposome formulations against biofilms of potentially pathogenic bacteria associated to corrosion isolated from the water of cooling towers from an oil refinery plant in Brazil. Antibiofilm assays with liposomes were performed in 96-wells microtiter plates, and data was compared to free chloramphenicol treatment. Chloramphenicol-loaded liposomes were successfully produced using the dehydration-rehydration method, with vesicle diameters of 131 nm (100 nm membrane extrusion) and 182 nm (200 nm membrane extrusion) assessed by dynamic light scattering. The liposomes obtained by 100 nm membrane extrusion were more effective than 200 nm membrane extrusion vesicles against the biofilms after overnight exposure, and the free drug had no antibiofilm effect. Our study open doors for more investigations on liposome entrapment of antimicrobial compounds such as biocides of industrial use, for controlling biofilm formation in aquatic environments.

      PubDate: 2017-03-16T15:11:35Z
      DOI: 10.1016/j.jsps.2017.03.003
  • Study of DNA damage caused by dipyrone in presence of some transition
           metal ions

    • Authors: Bruna Corrêa Roriz; Horacio Dorigan Moya
      Abstract: Publication date: Available online 27 February 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Bruna Corrêa Roriz, Horacio Dorigan Moya
      The DNA damage in the presence of dipyrone (used as its sodium salt, NaDip) and some transition metal ions in an air saturated ([O2] ≈ 0.25 mM) non-buffered solution at T = (25.0 ± 0.5)°C was investigated by agarose gel electrophoresis. As metal ions Cu2+, Fe3+, Ni2+ and Mn3+ were selected and evaluated in the present study because of the important role they play in a biological system. pUC19 plasmid DNA damage-induced by NaDip (80-600 μM) was observed in the presence of 100 μM Cu2+. The damage was proportional to the NaDip concentration provided that the order of addition of reagents (pUC19 plasmid DNA + Cu2+ + NaDip) is obeyed. Addition in the reaction medium of ligands for Cu2+ and Cu+, respectively EDTA and NC, promoted total inhibition or reduction of the pUC19 plasmid DNA damage suggesting the involvement of the Cu2+/Cu+ cycle. Besides, the decrease in the pUC19 plasmid DNA damage after addition of catalase (1.0×10-4 mg μL-1) in the same reaction medium indicates that H2O2 is also involved in the damage process. In NaDip concentration range (80-600 μM), and under same the experimental conditions, it was not possible to conclude whether there was pUC19 plasmid DNA damage caused by 10 μM Fe3+. No damage was observed in the presence of Mn3+ or Ni2+. Although the technique used in this study is sensitive to detect the pUC19 plasmid DNA damage it was not possible to identify in which DNA base this damage occurs. Further studies with other techniques should be made to unambiguously identify the oxidative intermediates that are responsible for the DNA damage. As far as we know, this is the first study dealing with the pUC19 plasmid DNA damage-induced by NaDip in presence of copper, iron, nickel and manganese ions.

      PubDate: 2017-03-03T21:41:06Z
      DOI: 10.1016/j.jsps.2017.02.010
  • Novel Essential Amino Acid-Sulfanilamide Hybrid as Safe Anti-ulcerogenic
           agent with Anti-Helicobacter pylori activity

    • Authors: Amani S.Awaad; Ahmed M. Alafeefy; Fatmah A.S. Alasmary; Reham M. El-Meligy; M.E. Zain; Saleh I. Alqasoumi
      Abstract: Publication date: Available online 27 February 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Amani S.Awaad, Ahmed M. Alafeefy, Fatmah A.S. Alasmary, Reham M. El-Meligy, M.E. Zain, Saleh I. Alqasoumi
      A novel and safe essential amino acid (Leucine) incorporating sulfanilamide was synthesized, and evaluated for its anti-ulcerogenic activity and in-vitro anti-Helicobacter pylori activity. The new molecule showed a dose dependent activity against absolute ethanol-induced ulcer in rats, it produced percent protection of control ulcer by 66.7 at dose 100 mg/kg. In addition it showed a potent anti-Helicobacter pylori activity in-vitro against 7 clinically isolated strains. The minimum inhibitory concentration (MIC) ranged from 12.5 to 50 µg/ml. The preliminary safety studies and toxicity profile are optimistic and encouraging.

      PubDate: 2017-03-03T21:41:06Z
      DOI: 10.1016/j.jsps.2017.02.012
  • X-ray crystallographic and validated HPTLC analysis of the biomarker
           chromone glucoside (schumanniofioside A) isolated from Acalypha Fruticosa
           growing in Saudi Arabia

    • Authors: Areej M. Al-Taweel; Ghada A. Fawzy; Shagufta Perveen; Perwez Alam; Ali A. El Gamal
      Abstract: Publication date: Available online 27 February 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Areej M. Al-Taweel, Ghada A. Fawzy, Shagufta Perveen, Perwez Alam, Ali A. El Gamal
      A chromone glucoside 2-methyl-5,7-dihydroxychromone 5-O-β-D-glucopyranoside (schumanniofioside A, compound 1) was isolated from the methanol extract of Acalypha fruticosa. The structure of compound 1 was fully assigned based on nuclear magnetic resonance (NMR) (1H, 13C and 2D) spectra andelectrospray ionization mass spectrum (ESI-MS) in addition to X-ray Crystallography. The molecules were packed in the crystal structure by eight intermolecular O–H …. O and C–H …. O interactions. The structure of compound 1 belongs to monoclinic, P21, a =9.1989 (4) Å, b = 4.6651 (2) Å, c =20.4042 (7) Å, β = 97.862 (3)°, V = 867.31 (6) Å3, Z = 2, wR ref (F 2 ) = 0.101, T = 100 K. Thus, the bond angles, bond lengths and absolute structure of compound 1 were confirmed by its X-ray structure. A validated HPTLC method was developed for the quantitative analysis of compound 1 in chloroform and methanol extracts of A. fruticosa. It was found to furnish a compact and sharp band of compound 1 at Rf= 0.13 ± 0.005 using chloroform, methanol and glacial acetic acid [17: 3: 0.5 (v/v/v)] as mobile phase. The LOD and LOQ for compound 1 were found to be 17.86 and 54.13 ng / band, respectively. Compound 1 was found in both chloroform and methanol extracts of the plant (0.03% w/w and 0.31% w/w, respectively). The proposed HPTLC method can be used for the further analysis of schumanniofioside A in different plant extracts, herbal formulations and biological samples as well as in process quality control.

      PubDate: 2017-03-03T21:41:06Z
      DOI: 10.1016/j.jsps.2017.02.011
  • Halloysite nanotubes as carriers of Vancomycin in alginate-based wound

    • Authors: Joanna Kurczewska; Paulina Pecyna; Magdalena Ratajczak; Marzena Gajęcka; Grzegorz Schroeder
      Abstract: Publication date: Available online 16 February 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Joanna Kurczewska, Paulina Pecyna, Magdalena Ratajczak, Marzena Gajęcka, Grzegorz Schroeder
      The influence of an inorganic support – halloysite nanotubes – on the release rate and biological activity of the antibiotic encapsulated in alginate-based dressings was studied. The halloysite samples were loaded with approx. 10 wt. % of the antibiotic and then encapsulated in Alginate and Gelatin/Alginate gels. The material functionalized with aliphatic amine significantly extended the release of vancomycin from alginate-based gels as compared to that achieved when silica was used. After 24 hours, the released amounts of the antibiotic immobilized at silica reached 70%, while for the drug immobilized at halloysite the released amount of vancomycin reached 44% for Alginate discs. The addition of gelatin resulted in even more prolonged sustained release of the drug. The antibiotic was released from the system with a double barrier with Higuchi kinetic model and Fickian diffusion mechanism. Only the immobilized drug encapsulated in Alginate gel demonstrated very good antimicrobial activity against various bacteria. The inhibition zones were greater than those of the standard discs for the staphylococci and enterococci bacteria tested. The addition of gelatin adversely affected the biological activity of the system. The inhibition zones were smaller than those of the reference samples. A reduction in the drug dose by half had no significant effect on changing the release rate and microbiological activity. The in vivo toxicity studies of the material with immobilized drug were carried out with Acutodesmus acuminatus and Daphnia magna. The material studied had no effect on the living organisms used in the bioassays. The proposed system with a double barrier demonstrated high storage stability.

      PubDate: 2017-02-17T01:57:10Z
      DOI: 10.1016/j.jsps.2017.02.007
  • Assessment of physical properties of granules with paracetamol and

    • Authors: Michal Szumilo; Piotr Belniak; Katarzyna Swiader; Ewelina Holody; Ewa Poleszak
      Abstract: Publication date: Available online 16 February 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Michal Szumilo, Piotr Belniak, Katarzyna Swiader, Ewelina Holody, Ewa Poleszak
      Caffeine increases the analgesic properties of acetaminophen and therefore it is reasonable to use both substances together in one drug form in stronger pain. Currently, there are no commercially available pharmaceutical combination products containing acetaminophen and caffeine, which is present as granules. The aim of the study was to obtain twelve different granules with these therapeutic substances and determine the effect of various excipients on the quality of the drug form. All the granules were made by wet granulation. Two types of binders were used: polyethylene glycol 6000 (PEG) and polyvinylpyrrolidone K30 (PVP) as well as different types of fillers. The physical properties of granules were assessed in accordance to the requirements of the European Pharmacopoeia 8th ed. The highest apparent density was found in preparations containing calcium hydrophosphate (0.609 g/mL) and the lowest - containing mannitol (0.353 g/mL) as a filler. The Hausner ratio of most prepared granules ranged from 1.05 to 1.11, while the compressibility index ranged from 4.59 to 10.48%. The evaluation of properties of individual granules helped to indicate formulation with good features, which perhaps will be a good alternative to currently available painkillers with caffeine and acetaminophen.

      PubDate: 2017-02-17T01:57:10Z
      DOI: 10.1016/j.jsps.2017.02.009
  • Synthetic detergents: 100 years of history

    • Authors: Ana Carolina Kogawa; Beatriz Gamberini Cernic; Leandro Giovanni Domingos do Couto; Hérida Regina Nunes Salgado
      Abstract: Publication date: Available online 14 February 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Ana Carolina Kogawa, Beatriz Gamberini Cernic, Leandro Giovanni Domingos do Couto, Hérida Regina Nunes Salgado
      In the year 2016 the synthetic detergents complete 100 years and in this story they evolved as cleaners. They are already part of the routine of thousands of people worldwide. For a higher power of cleaning of the detergent, today, are added phosphates, the main responsible for environmental problems. After 100 years of synthetic detergents, the effect of the combination of various cleaners on the environment is a gap. Legislation and guidelines about the other components of the formula of cleaners still missing. Even the term biodegradable can be best placed on the diversity of products currently entitled biodegradable. A lot attitudes can still be taken to continuously improve the relationship between the parties involved, animals, plants, waters and men, so that in another 100 years continues to exist this interaction with the environment without destroying it. The marketing used by synthetic detergent companies evolved a lot over the years and showed maturity to deal with changes in theories and strategies for promotion and even with the constant social reform that its consumer lived, accompanying them intelligently to be able to capture their changing needs and desires, and so assemble the best way to connect to them. This paper focuses on the subject synthetic detergents as well as (i) types and applications, (ii) threats, (iii) sustainability, (iv) legislation, (v) packaging and (vi) marketing strategies.

      PubDate: 2017-02-17T01:57:10Z
      DOI: 10.1016/j.jsps.2017.02.006
  • The Effect of Metformin Use on Pregnancy Rates among Polycystic Ovary
           Syndrome Patients Undergoing In Vitro Fertilization: A
           Retrospective-Cohort Study

    • Authors: Yazed Sulaiman Al-Ruthia; Hazem Al-Mandeel; Hisham AlSanawi; Bander AlBalkhi; Wael Mansy; Reem AlGasem; Lama AlMutairi
      Abstract: Publication date: Available online 14 February 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Yazed Sulaiman Al-Ruthia, Hazem Al-Mandeel, Hisham AlSanawi, Bander AlBalkhi, Wael Mansy, Reem AlGasem, Lama AlMutairi
      Background Metformin is widely used with gonadotropins by women with polycystic ovary syndrome (PCOS) during in vitro fertilization (IVF) to increase their chances of pregnancy. The aim of this study was to evaluate the efficacy of metformin in improving the rates of clinical pregnancy among women with PCOS undergoing IVF. Methods This was a retrospective cohort study of women with PCOS, aged 18–40 years, undergoing IVF during 2006–2012 at a university hospital in Riyadh, Saudi Arabia. Baseline patient data including menstrual frequency, biochemical parameters such as fasting serum insulin (FSI) concentration, comorbidities, and the rates of ovulation and pregnancy were collected. Pregnancy rates were compared between the metformin and non-metformin groups. Results A total of 210 women with PCOS met the inclusion criteria and were included in the study. Of the 210 women with PCOS, 109 of them received metformin in addition to gonadotropins. Patients who received metformin were 16% less likely to be pregnant in comparison with those who did not receive metformin (OR = 0.840; 95% CI = 0.710–0.993; P = 0.0415), when controlled for baseline prolactin level, testosterone level, lipid panel, FSI concentration, fasting plasma glucose (FPG) concentration, comorbidities, duration of infertility, daily metformin dosage, and the previous use of clomiphene and/or leuprolide. Conclusions Metformin co-treatment during IVF may negatively affect pregnancy rates. Further well-designed, randomized, double-blind placebo-control clinical trials are needed to confirm the findings of this study.

      PubDate: 2017-02-17T01:57:10Z
      DOI: 10.1016/j.jsps.2017.02.008
  • Standardization of clinical pharmacist’s activities: methodology

    • Authors: Jana Gregorová; Jitka Rychlíčková; Jan Šaloun
      Abstract: Publication date: Available online 14 February 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Jana Gregorová, Jitka Rychlíčková, Jan Šaloun
      Study objectives Establishing standardized and controlled system of work at a clinical pharmacy department and establishing effective recording of activities of a group of four clinical pharmacist when providing clinical pharmaceutical care (CPC) in a hospital. Methods The duration of evaluated period is 5.5 years. The first part was defining the purpose, methods and activities of clinical pharmaceutical care, the next part was designing the software for recording patient’s data and CPC activities. To verify the functionality of our system the third part was conducted (from January 1, 2015 to June 30, 2015). Results CPC activities were defined precisely. During the 6 months period, 3946 patients were reviewed (17% of patients admitted), in this group, 41% patients was labeled as risk (these patients had one or more risk factor). 1722 repeated reviews were performed, 884 drug therapeutic recommendations were recorded. The calculated average time necessary for one CPC activity is 28 minutes. Conclusion During the 5 year period, standardized system of work in clinical pharmacy department was established. This system is based on clearly defined activities and it enables external control. Our results supply data for negotiations with health insurance companies.

      PubDate: 2017-02-17T01:57:10Z
      DOI: 10.1016/j.jsps.2017.02.005
  • Preparation, characterization, and in vitro diffusion study of nonwoven
           electrospun nanofiber of curcumin-loaded cellulose acetate phthalate

    • Authors: Rramaswamy Ravikumar; Mani Ganesh; Udumansha Ubaidulla; Eun Young Choi; Hyun Tae Jang
      Abstract: Publication date: Available online 12 February 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Rramaswamy Ravikumar, Mani Ganesh, Udumansha Ubaidulla, Eun Young Choi, Hyun Tae Jang
      Novel curcumin (CUR)-loaded cellulose acetate phthalate (CAP) nonwoven electrospun nanofiber (NF) transdermal mat was developed and evaluated for its in vitro CUR diffusion properties. Various CAP solutions from 5–20 wt% were tested; 17.5 wt% was found to be a suitable concentration for NF fabrication without defects, such as bubble or ribbon structures. The selected wt% CAP solution was loaded with CUR and electrospun into NFs. The prepared CUR-loaded NFs were characterized using scanning electron microscopy, X-ray diffraction, ultraviolet-visible spectroscopy, thermogravimetric analysis (TGA), and in vitro diffusion studies. The as-prepared fibers demonstrated controlled in vitro transdermal delivery of CUR for up to 24 h.

      PubDate: 2017-02-17T01:57:10Z
      DOI: 10.1016/j.jsps.2017.02.004
  • Prevalence of self-medication practice with herbal products among
           non-psychotic psychiatric patients from southeastern Serbia: a
           cross-sectional study

    • Authors: Nikola M. Stojanović; Ljiljana Samardžić; Pavle J. Randjelović; Niko S. Radulović
      Abstract: Publication date: Available online 10 February 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Nikola M. Stojanović, Ljiljana Samardžić, Pavle J. Randjelović, Niko S. Radulović
      The aim of this study was to evaluate the usage prevalence of herbal products (HP) and to ascertain the identity, mode and adverse effects of plant taxa used in self-medication practice for anxiety, depression and insomnia in patients with non-psychotic disorders originating from southeastern Serbia. Also, we compared HP users and non-users on the variables of socio-demographic characteristics, information source and origin of HP. The study was done by a face-to-face interview with a trained psychiatrist using a structured questionnaire administered to 136 adult patients suffering from non-psychotic mental disorders. A typical herbal-product user among non-psychotic psychiatric patients from southeastern Serbia is a middle-aged married woman, with a secondary level of education, unemployed and living in an urban area. Non-psychotic psychiatric patients, although not living predominantly in rural areas, were familiar with a variety of ethno-medicines and were often using HP primarily without the consultation of their psychiatrists/physicians. HP stated to be most frequently used for psychiatry-related symptoms included: Melissa officinalis, Mentha x piperita, Hypericum perforatum and Valeriana officinalis. The interviewees rarely stated adverse reactions related to the HP usage; however, this should not be generalized, since HP are known to vary in the content of their adverse reaction-causing constituents.

      PubDate: 2017-02-11T00:35:24Z
      DOI: 10.1016/j.jsps.2017.02.002
  • The extent of use of online pharmacies in Saudi Arabia

    • Authors: Norah Abanmy
      Abstract: Publication date: Available online 10 February 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Norah Abanmy
      Purpose Online pharmacies sell medicine over the Internet and deliver them by mail. The main objective of this study is to explore the extent of use of online pharmacies in Saudi Arabia which will be useful for the scientific community and regulators. Methods An Arabic survey questionnaire was developed for this study. The questionnaire was distributed via email and social media. Four sections were created to cover the objectives: experience with online shopping in general, demographics, awareness of the existence and customer experiences of buying medicine online, and reasons for buying/not buying medicine online. Results A total of 633 responses were collected. Around 69% (437) of them were female and the majority (256, 40.4%) was in the age range 26–40. Only 23.1% (146) were aware of the existence of online pharmacies where 2.7% (17) of them had bought a medicine over the Internet and 15 (88.2%) respondents out of the 17 was satisfied with the process. Lack of awareness of the availability of such services was the main reason for not buying medicines online. Many respondents (263, 42.7%) were willing to try an online pharmacy, although majorities (243, 45.9%) were unable to differentiate between legal and illegal online pharmacies. The largest categories of products respondents were willing to buy them online were nonprescription medicines and cosmetics. Conclusion The popularity of purchasing medicines over the Internet is still low in Saudi Arabia. However, because the majority of respondents are willing to purchase medicines online, efforts should be made by the Saudi FDA to set regulations and monitor this activity.

      PubDate: 2017-02-11T00:35:24Z
      DOI: 10.1016/j.jsps.2017.02.001
  • Synthesis, Molecular Modeling and Anticancer Activity of New Coumarin
           Containing Compounds

    • Authors: Shaimaa A. Morsy; Abdelbasset A. Farahat; Magda N.A. Nasr; Atif S. Tantawy
      Abstract: Publication date: Available online 10 February 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Shaimaa A. Morsy, Abdelbasset A. Farahat, Magda N.A. Nasr, Atif S. Tantawy
      A series of new coumarin containing compounds were synthesized from 4-bromomethylcoumarin derivatives 2a, b and different heteroaromatic systems 4a-e, 6a-d, 8, 10 via methylene thiolinker. Twenty four compounds were screened biologically against two human tumor cell lines, breast carcinoma MCF-7 and hepatocellular carcinoma HePG-2, at the national cancer institute, Cairo, Egypt using 5-fluorouracil as standard drug. Compounds 5h, 7d, 7h, 9a, 13a and 13d showed strong activity against both MCF-7 and HepG-2 cell lines with being compound 13a is the most active with IC50 values of 5.5 µg/ml and 6.9 µg/ml respectively. Docking was performed with protein 1KE9 to study the binding mode of the designed compounds.

      PubDate: 2017-02-11T00:35:24Z
      DOI: 10.1016/j.jsps.2017.02.003
  • A Quality by Design approach for the development of lyophilized liposomes
           with simvastatin

    • Authors: Alina Porfire; Dana Maria Muntean; Lucia Rus; Bianca Sylvester; Ioan Tomuţă
      Abstract: Publication date: Available online 9 February 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Alina Porfire, Dana Maria Muntean, Lucia Rus, Bianca Sylvester, Ioan Tomuţă
      Lyophilization is used to ensure an increased shelf-life of liposomes, by preserving them in dry state, more stable than the aqueous dispersions. When stored as aqueous systems, the encapsulated drugs are released and the liposomes might aggregate or fuse. The aim of this study was to develop and optimize a lyophilized formulation of simvastatin (SIM) loaded into long circulating liposomes using the Quality by Design (QbD) approach. Pharmaceutical development by QbD aims to identify characteristics that are critical for the final product quality, and to establish how the critical process parameters can be varied to consistently produce a product with the desired characteristics. In the case of lyophilized liposomes, the choice of the optimum formulation and technological parameters has to be done, in order to protect the integrity of the liposomal membrane during lyophilization. Thus, the influence of several risk factors (3 formulation factors: PEG proportion, cholesterol concentration, the cryoprotectant to phospholipids molar ratio, and 2 process parameters: the number of extrusions through 100 nm polycarbonate membranes and the freezing conditions prior lyophilization) over the critical quality attributes (CQAs) of lyophilized long circulating liposomes with simvastatin (lyo-LCL-SIM), i.e. the size, the encapsulated SIM concentration, the encapsulated SIM retention, the Tm change and the residual moisture content, was investigated within the current study using the design of experiments tool of QbD. Moreover, the design space for lyo-LCL-SIM was determined, in which the established quality requirements of the product are met, provided that the risk factors vary within the established limits.

      PubDate: 2017-02-11T00:35:24Z
      DOI: 10.1016/j.jsps.2017.01.007
  • Formulation and characterization of novel soft lipid-based nanoparticles
           for enhanced transdermal delivery of eprosartan mesylate

    • Authors: Abdul Ahad; Abdulmohsen A. Al-Saleh; Abdullah M. Al-Mohizea; Fahad I. Al-Jenoobi; Mohammad Raish; Alaa Eldeen B. Yassin; Mohd Aftab Alam
      Abstract: Publication date: Available online 2 February 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Abdul Ahad, Abdulmohsen A. Al-Saleh, Abdullah M. Al-Mohizea, Fahad I. Al-Jenoobi, Mohammad Raish, Alaa Eldeen B. Yassin, Mohd Aftab Alam
      The objective of the present work was to formulate, optimize and evaluate the potential of novel soft lipid-based nanoparticles i.e. nano-transfersomes, containing eprosartan mesylate (EM) for transdermal delivery. Nano-transfersomes of EM were developed using Phospholipon 90G, Span 80 (SP) and sodium deoxycholate (SDC) and characterized for vesicle size, shape, entrapment efficiency, in vitro skin permeation study and confocal laser scanning microscopy. The optimized nano-transfersomes formulation showed vesicles size of 108.53 ± 0.06 nm and entrapment efficiency of 63.00 ± 2.76%. The optimized nano-transfersomes provided an improved transdermal flux of 27.22 ± 0.29 µg/cm2/h with an enhancement ratio of 16.80 over traditional liposomes through Wistar rat skin. Confocal laser microscopy of rat skin treated with the optimized formulation showed that the formulation was eventually distributed and permeated deep into the rat skin. The present investigation has shown that the nature and concentration of surfactants (edge activators) influence immense control on the characteristics of nano-transfersomes. It was concluded that the developed nano-transfersomes surmount the limitation of low penetration ability of the traditional liposomes across the rat skin. Improved drug delivery presented by nano-transfersomes establishes this system as an encouraging dosage form for the delivery of EM via skin route.

      PubDate: 2017-02-04T22:48:54Z
      DOI: 10.1016/j.jsps.2017.01.006
  • Adverse drug reactions in high-risk pregnant women: A prospective study

    • Authors: Alfredo Dias de Oliveira-Filho; Antonio Emanuel Soares Vieira; Roberta Cruz da Silva; Sabrina Joany Felizardo Neves; Thiago Antonio Barros Gama; Ryane Vieira Lima; Wlisses Ramon Oliveira; Júlia Maria de Gonçalves Dias
      Abstract: Publication date: Available online 2 February 2017
      Source:Saudi Pharmaceutical Journal
      Author(s): Alfredo Dias de Oliveira-Filho, Antonio Emanuel Soares Vieira, Roberta Cruz da Silva, Sabrina Joany Felizardo Neves, Thiago Antonio Barros Gama, Ryane Vieira Lima, Wlisses Ramon Oliveira, Júlia Maria de Gonçalves Dias
      BACKGROUND Because pregnant women are often excluded from clinical trials, there is still very limited information about the risk and safety of prescription drugs during pregnancy. OBJECTIVE We aimed to determine the prevalence of Adverse Drug Reactions (ADRs) in high-risk pregnant women after hospital admission. A prospective study was carried out in a teaching maternity hospital in Brazil during six months. Causality of ADRs was assessed through the Naranjo Algorithm and Korean Algorithm for ADR Causality Assessment. Severity of ADRs was assessed using Hartwig’s Severity Assessment Scale. RESULTS The prevalence of ADRs among the 294 inpatients studied was 8.8%. The mean age was 27.14 (±7.5) y.o. Patients's age was related to the presence of ADRs, while the manifestation of these events was not associated with any adverse pregnancy outcome. 75.9% of the ADRs reported in the study were of mild severity and 24.1% were of moderate severity. No ADR was caused by drug-drug interaction, however a significant increase in blood pressure was observed in all patients using concurrent methyldopa and ferrous sulfate. CONCLUSION Overall, ADRs were not common events among high-risk pregnant women and no adverse pregnancy outcomes following these events were observed.

      PubDate: 2017-02-04T22:48:54Z
      DOI: 10.1016/j.jsps.2017.01.005
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