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  Subjects -> PHARMACY AND PHARMACOLOGY (Total: 560 journals)
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Journal Cover Saudi Pharmaceutical Journal
  [SJR: 0.417]   [H-I: 14]   [0 followers]  Follow
    
  This is an Open Access Journal Open Access journal
   ISSN (Print) 1319-0164
   Published by Elsevier Homepage  [2969 journals]
  • An overview of pharmacodynamic modelling, ligand-binding approach and its
           application in clinical practice

    • Abstract: Publication date: Available online 9 July 2016
      Source:Saudi Pharmaceutical Journal
      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: 2016-07-27T08:51:23Z
       
  • Biochemical and molecular modulation of CCl4-induced peripheral and
           central damage by Tilia americana var. mexicana extracts

    • Abstract: Publication date: Available online 12 July 2016
      Source:Saudi Pharmaceutical Journal
      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 (100 mg/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: 2016-07-27T08:51:23Z
       
  • Editorial Board

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4




      PubDate: 2016-07-27T08:51:23Z
       
  • Temperature excursion management – A novel approach of quality
           system in pharmaceutical industry

    • Abstract: Publication date: Available online 9 July 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Nirmal Kumar, Ajey Jha
      Quality of pharmaceutical product largely depends upon by 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 an d 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: 2016-07-27T08:51:23Z
       
  • Pain and anxiety management for pediatric dental procedures using various
           combinations of sedative drugs: A review

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Giath Gazal, Wamiq Musheer Fareed, Muhammad Sohail Zafar, Khalid H. Al-Samadani
      For fearful and uncooperative children behavioral management techniques are used. In order to control the pain and anxiety in pedodontic patients, pharmacologic sedation, anesthesia and analgesia are commonly used. Midazolam is commonly used as an oral sedation agent in children; it has several features such as safety of use, quick onset and certain degree of amnesia that makes it a desirable sedation agent in children. This review paper discusses various aspects of oral midazolam, ketamine and their combinations in conscious sedation including, advantages of oral route of sedation, pharmacokinetics, range of oral doses, and antagonists for clinical dental treatment procedures.


      PubDate: 2016-07-27T08:51:23Z
       
  • Drug nanocrystals: A way toward scale-up

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Kale Mohana Raghava Srivalli, Brahmeshwar Mishra
      Drug nanocrystals comprise unique drug delivery platforms playing a significantly important and distinctive role in drug delivery and as such, the industry and academia are spending a lot of their time and money in developing the nanocrystal products. The current research works in this field depict a vivid shift from lab scale optimization studies to scale up focused studies. In this emerging scenario of nanocrystal technology, a review on some exemplary and progressing research studies with either scalability as their objective or upscaling as their future scope may smoothen the future upscaling attempts in this field. Hence, this paper reviews the efforts of such research works as case studies since an analysis of such research studies may input certain beneficial knowledge to carry out more scale up based research works on nanocrystals.


      PubDate: 2016-07-27T08:51:23Z
       
  • Drug safety: The concept, inception and its importance in patients’
           health

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Thamir M. Alshammari
      Background Drug safety is one of the hottest topics in daily medical practice, particularly with regard to approving new medication or questioning the possibility of withdrawing a drug from the market. Aim The aim of this review is to highlight the importance of the drug safety concept and its impact on patients’ health. Methods A literature search was conducted using Pubmed®, EMBASE®, EBSCO and Medline in the period between 1980 and 2013. The terms used in the search included “Drug Safety”, “Medication Safety”, “Patient Safety”, “Drug Interaction”, “Drug Pharmacokinetic”, and “Adverse Drug Reaction”. All retrieved abstracts were evaluated within the context of the review objectives. The full texts of the selected articles were included in this review. Studies in non-English language were excluded in this review. Results Since the early days of the past century, many acts, laws, or amendments have been created to make sure that approved drugs are first safe and then effective. Furthermore, these regulations are continuing to change to make sure that these drugs have a positive benefit–risk balance. Personalized medicine should be considered when medications are given to patients because the pharmacokinetic process inside the body varies from patient to patient and from one specific disease state to another. However, adverse drug reactions can be minimized if more precautions are taken by healthcare professionals, especially including the patient as one pillar of the therapeutic plan and providing more patient counseling, which will improve drug safety. Conclusion The drug safety concept has earned a lot of attention during the past decade due to the fact it plays a major role in patients’ health. Recent laws stress this concept should be included in the process of new medications’ approval and continued conduct of post-marketing drug evaluations. Benefit–risk assessment should be considered by all health care professionals when they need to give specific drugs to specific groups of patients. Therefore, more care should be given to some patients, such as pregnant women, children and the elderly, since they are considered vulnerable populations.


      PubDate: 2016-07-27T08:51:23Z
       
  • A review on the strategies for oral delivery of proteins and peptides and
           their clinical perspectives

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Abdul Muheem, Faiyaz Shakeel, Mohammad Asadullah Jahangir, Mohammed Anwar, Neha Mallick, Gaurav Kumar Jain, Musarrat Husain Warsi, Farhan Jalees Ahmad
      In the modern world, a number of therapeutic proteins such as vaccines, antigens, and hormones are being developed utilizing different sophisticated biotechnological techniques like recombinant DNA technology and protein purification. However, the major glitches in the optimal utilization of therapeutic proteins and peptides by the oral route are their extensive hepatic first-pass metabolism, degradation in the gastrointestinal tract (presence of enzymes and pH-dependent factors), large molecular size and poor permeation. These problems can be overcome by adopting techniques such as chemical transformation of protein structures, enzyme inhibitors, mucoadhesive polymers and permeation enhancers. Being invasive, parenteral route is inconvenient for the administration of protein and peptides, several research endeavors have been undertaken to formulate a better delivery system for proteins and peptides with major emphasis on non-invasive routes such as oral, transdermal, vaginal, rectal, pulmonary and intrauterine. This review article emphasizes on the recent advancements made in the delivery of protein and peptides by a non-invasive (peroral) route into the body.


      PubDate: 2016-07-27T08:51:23Z
       
  • Neonatal parenteral nutrition: Review of the pharmacist role as a
           prescriber

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Mohamed H. Ragab, Mohammed Y. Al-Hindi, Meshari M. Alrayees
      Introduction In the context of the continuous quest to improve the care of the neonates especially the critically ill premature infants, the extended role of pharmacists in the process of parenteral nutrition order writing and effective participation in decision-making especially in the neonatal population is increasingly important. This review aims to present results from the literature review of available evidence on the pharmacist role in neonatal parenteral nutrition therapy. Material and methods Key medical, clinical, and review databases were searched; relevant articles were retrieved and evaluated. Results and discussion A total of 19 papers out of 7127 searched papers met the criteria for inclusion, discussing the review topic. The main focus of the selected papers was on parenteral nutrition practice as related to the pharmacy practice. The overall quality of studies was mixed. Conclusion Overall, the review presents the up-to-date status of the most recent analysis being undertaken on the topic of pharmacist involvement in the parenteral nutrition order writing practices and more specific in the neonatal population over the period from 1979 to 2013. The overall impression is that the practice of pharmacist writing neonatal parenteral nutrition orders already exists, but still limited if compared with the practice of pharmacist writing adult parenteral nutrition orders which is much more established in many countries. There was no single clinical study evaluating this practice, as we were able to retrieve only two surveys, which make it difficult to evaluate the pharmacist role in this area. Nevertheless, despite the wide variation in literature types, characteristics and quality, there are consistent patterns across all the reviewed literatures that competencies of the pharmacist in this field are well represented, which make it very important to carry out good quality clinical studies in this field. Finally, we are currently conducting a prospective clinical study to evaluate the impact of clinical pharmacist as a neonatal PN prescriber, this impact will be judged through the study outcomes as reducing the metabolic and electrolyte complications and increasing the mean daily weight gain during PN therapy and reducing the average number of days of PN till enteral feeding is achieved.


      PubDate: 2016-07-27T08:51:23Z
       
  • An evolving role of clinical pharmacists in managing diabetes: Evidence
           from the literature

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Samia Alhabib, Maha Aldraimly, Ali Alfarhan
      Background Diabetes mellitus is a rapidly growing disease world-wide that is estimated to be present in 6.6% of the international population and projected to be increased by 7.8% in 2030. Treating diabetic patients is multifaceted in all aspects and they require objectives and optimum information in order to obtain the maximum benefits of their treatment and avoid complications. Pharmacists are increasingly considered as a part of the health care system. Hence, the aim of this review is to address and summarize the effectiveness of clinical pharmacists in managing diabetic patients. Method This is a narrative review of the evidence from the literature in order to answer the present question of what is the evidence of the role of clinical pharmacists in managing diabetic patients. We searched five databases including: the Cochrane library, MEDLINE, EMBASE, TRIP, and Science Direct. We will also try to look for other potentially eligible trials or ancillary publications by searching the reference lists of retrieved included trials, (systematic) reviews, meta-analyses and health technology assessment reports. Outcomes included short-term and long-term measures. Results Final search revealed nine studies. They were heterogeneous in terms of interventions, participants, settings and outcomes. Studies varied in their quality and/or reporting of their findings conducted in several settings. Majority of the studies were conducted in Western countries, one in Hong Kong and one in South India. In majority of the studies, pharmacists’ role was mainly to specify all drug-related problems including poor drug compliance and side effects and communicating these to the physician. We found that those who received the pharmacist care had a statistically significant reduction in coronary heart disease, blood pressure, HA1c, quality of life and lipid profile. Conclusion Our review demonstrated the important role of clinical pharmacists in managing diabetic patients at diverse settings worldwide. There is an urgent need to recognize and change regulations to allow shared practice agreements among physicians, pharmacists, and other allied health professionals. These mutual agreements would allow more streamlined provision of health care delivery from non-physician health professionals to participants with common health conditions.


      PubDate: 2016-07-27T08:51:23Z
       
  • Evidence-based pharmaceutical care: The next chapter in pharmacy practice

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Osama Mohammad Al-Quteimat, Amer Mostafa Amer
      Introduction Pharmacy is a very dynamic profession and the role of the pharmacist is improving with the expansion of the scope of services and the introduction of new subspecialties over time. Moving from being medication dispensers to outcome-oriented and patient-focused care providers; pharmacists will carry more responsibility and commitment to improve their knowledge and practice. Being updated and evidence-based is a key tool to achieve effective pharmaceutical care services. The primary purpose of this article is to highlight the concept of “evidence based pharmaceutical care” as professional practice to improve the quality of pharmaceutical care. Methods Literature for relevant evidence was searched by Medline (through PubMed), Cochrane library using the keywords: pharmaceutical care, evidence-based and pharmacy practice. Also a manual search through major journals for articles referenced in those located through PubMed was done. Results and discussion There is strong data showing that pharmaceutical care lead to improvement in health outcomes and cost-effective therapy. More efforts, policies and qualified staff are needed to establish the “evidence-based pharmaceutical care” as new daily professional practice. Evidence to support pharmacists in their emerging role as care providers is available to improve the efficacy and quality of pharmaceutical care. Education and specialized training practicing evidence based approach are vital to prepare pharmacists to provide high quality pharmaceutical care. Conclusion As care providers, pharmacists are effective in providing high quality patient care and being members in multidisciplinary clinical teams is needed to give them the opportunity. Evidence based pharmaceutical care is a natural and logical emerging concept in the modern pharmacy practice to achieve high quality and more effective pharmaceutical care but still more efforts and resources are needed to promote new attitude toward more professional career.


      PubDate: 2016-07-27T08:51:23Z
       
  • Microemulgel: an overwhelming approach to improve therapeutic action of
           drug moiety

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Kalpesh C. Ashara, Jalpa S. Paun, M.M. Soniwala, J.R. Chavda, Vishal P. Mendapara, Nitin M. Mori
      As compared to gel and other topical preparations microemulgel has been prepared by screening of oils, emulsifier, and co-emulsifier on bases of solubility of an API in it. An API has high solubility and oil may also have more or less pharmacological property, so it may assist the therapeutic action of API. Due to presence of oil portion, it leads to more penetration of API in the skin. Oil Micelle Size was less than 500nm which provides more area for absorption of API in the skin so more penetration and more effective than macro-emulsion. Microemulgel has an advantage of emulgel that has dual benefits of micro-emulsion and gel and several other desirable properties like good consistency, thyrotrophic, greaseless, easily spreadable as well as removable, emollient, non-staining, water soluble, longer shelf-life, bio-friendly, transparent, pleasant appearance, ability of patients for self-medication, termination of medications will be easy, etc.


      PubDate: 2016-07-27T08:51:23Z
       
  • Microparticles as controlled drug delivery carrier for the treatment of
           ulcerative colitis: A brief review

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Nidhi, Muzamil Rashid, Veerpal Kaur, Supandeep Singh Hallan, Saurabh Sharma, Neeraj Mishra
      Ulcerative colitis is the chronic relapsing multifactorial gastrointestinal inflammatory bowel disease, which is characterized by bloody or mucus diarrhea, tenesmus, bowel dystension, anemia. The annual incidence of ulcerative colitis in Asia, North America and Europe was found to be 6.3, 19.2 and 24.3 per 100,000person-years. The major challenge in the treatment of ulcerative colitis is appropriate local targeting and drug related side-effects. To overcome these challenges, microparticulate systems seem to be a promising approach for controlled and sustained drug release after oral administration. The main goal of this article is to explore the role of microparticles in ulcerative colitis for the appropriate targeting of drugs to colon. There are different approaches which have been studied over the last decade, including prodrugs, polymeric approach, time released system, pH sensitive system, which show the site specific drug delivery to colon. Among these approaches, microparticulate drug delivery system has been gaining an immense importance for local targeting of drug to colon at a controlled and sustained rate. Combined approaches such as pH dependent and time dependent system provide the maximum release of drug into colon via oral route. This article embraces briefly about pathophysiology, challenges and polymeric approaches mainly multiparticulate systems for site specific drug delivery to colon in sustained and controlled manner so that drug related side-effects by reducing dosage frequency can be minimized.


      PubDate: 2016-07-27T08:51:23Z
       
  • Biosynthesis of metallic nanoparticles using plant derivatives and their
           new avenues in pharmacological applications – An updated report

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Palaniselvam Kuppusamy, Mashitah M. Yusoff, Gaanty Pragas Maniam, Natanamurugaraj Govindan
      The field of nanotechnology mainly encompasses with biology, physics, chemistry and material sciences and it develops novel therapeutic nanosized materials for biomedical and pharmaceutical applications. The biological syntheses of nanoparticles are being carried out by different macro–microscopic organisms such as plant, bacteria, fungi, seaweeds and microalgae. The biosynthesized nanomaterials have been effectively controlling the various endemic diseases with less adverse effect. Plant contains abundant natural compounds such as alkaloids, flavonoids, saponins, steroids, tannins and other nutritional compounds. These natural products are derived from various parts of plant such as leaves, stems, roots shoots, flowers, barks, and seeds. Recently, many studies have proved that the plant extracts act as a potential precursor for the synthesis of nanomaterial in non-hazardous ways. Since the plant extract contains various secondary metabolites, it acts as reducing and stabilizing agents for the bioreduction reaction to synthesized novel metallic nanoparticles. The non-biological methods (chemical and physical) are used in the synthesis of nanoparticles, which has a serious hazardous and high toxicity for living organisms. In addition, the biological synthesis of metallic nanoparticles is inexpensive, single step and eco-friendly methods. The plants are used successfully in the synthesis of various greener nanoparticles such as cobalt, copper, silver, gold, palladium, platinum, zinc oxide and magnetite. Also, the plant mediated nanoparticles are potential remedy for various diseases such as malaria, cancer, HIV, hepatitis and other acute diseases.


      PubDate: 2016-07-27T08:51:23Z
       
  • Dilemmas of the causality assessment tools in the diagnosis of adverse
           drug reactions

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Lateef M. Khan, Sameer E. Al-Harthi, Abdel-Moneim M. Osman, Mai A. Alim A. Sattar, Ahmed S. Ali
      Importance: Basic essence of Pharmacovigilance is prevention of ADRs and its precise diagnosis is crucially a primary step, which still remains a challenge among clinicians. Objective: This study is undertaken with the objective to scrutinize and offer a notion of commonly used as well as recently developed methods of causality assessment tools for the diagnosis of adverse drug reactions and discuss their pros and cons. Evidence review: Overall 49 studies were recognized for all assessment methods with five major decisive factors of causality evaluation, all the information regarding reasons allocating causality, the advantages and limitations of the appraisal methods were extracted and scrutinized. Findings: From epidemiological information a past prospect is designed and subsequent possibility merged this background information with a clue in the individual case to crop up with an approximation of causation. Expert judgment is typically based on the decisive factor on which algorithms are based, nevertheless in imprecise manner. The probabilistic methods use the similar principle; however connect probabilities to each measure. Such approaches are quite skeptical and liable to generate cloudy causation results. Causation is quite intricate to ascertain than correlation in Pharmacovigilance due to numerous inherent shortcomings in causality assessment tools. Conclusions and relevance: We suggest that there is a need to develop a high quality assessment tool which can meticulously establish suitable diagnostic criteria for ADRs with universal acceptance to improvise the fundamental aspect of drug safety and evade the impending ADRs with the motive to convert Pharmacovigilance into a state of art.


      PubDate: 2016-07-27T08:51:23Z
       
  • Hyperphosphatemia Management in Patients with Chronic Kidney Disease

    • Abstract: Publication date: July 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 4
      Author(s): Ahmed M. Shaman, Stefan R. Kowalski
      Hyperphosphatemia in chronic kidney disease (CKD) patients is a potentially life altering condition that can lead to cardiovascular calcification, metabolic bone disease (renal osteodystrophy) and the development of secondary hyperparathyroidism (SHPT). It is also associated with increased prevalence of cardiovascular diseases and mortality rates. To effectively manage hyperphosphatemia in CKD patients it is important to not only consider pharmacological and nonpharmacological treatment options but also to understand the underlying physiologic pathways involved in phosphorus homoeostasis. This review will therefore provide both a background into phosphorus homoeostasis and the management of hyperphosphatemia in CKD patients. In addition, it will cover some of the most important reasons for failure to control hyperphosphatemia with emphasis on the effect of the gastric pH on phosphate binders efficiency.


      PubDate: 2016-07-27T08:51:23Z
       
  • Effect of Pelargonidin isolated from Ficus benghalensis L. on phenotypic
           changes in zebrafish (Danio rerio) embryos

    • Abstract: Publication date: Available online 1 July 2016
      Source:Saudi Pharmaceutical Journal
      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: 2016-07-27T08:51:23Z
       
  • Development and characterization of methoxy poly(ethylene
           oxide)-block-poly(ε-caprolactone) (PEO-b-PCL) micelles as vehicles
           for the solubilization and delivery of tacrolimus

    • Abstract: Publication date: Available online 1 July 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Raisuddin Ali, Abubakar Farah, Ziyad Binkhathlan
      Tacrolimus is a potent immunosuppressant; however, it suffers from several problems such as poor water solubility (4–12μg/mL), low and variable oral bioavailability in patients, and narrow therapeutic window that could not be solved by the currently available i.v. formulation (Prograf®). Moreover, Prograf® contains HCO-60 (PEGylated castor oil) as a surfactant, which is reported to cause several side effects including hypersensitivity reactions. Therefore, the aim of the present study was to investigate the potential of PEO-b-PCL polymeric micelles as alternative vehicles for the solubilization and delivery of tacrolimus. Four PEO-b-PCL block copolymers, with different molecular weights of PCL, were synthesized by ring opening polymerization of ε-caprolactone using methoxy polyethylene oxide (5,000gmol−1) as initiator and stannous octoate as catalyst. Synthesized copolymers were characterized for their average molecular weights and polydispersity index by 1H NMR and gel permeation chromatography (GPC), respectively. Drug-free micelles of PEO-b-PCL were prepared through a co-solvent evaporation method using acetone as the organic co-solvent. Tacrolimus-loaded micelles were prepared using the same method with different initial amounts of drug. Prepared micelles were characterized for their mean diameter size and polydispersity of the micellar population by dynamic light scattering, and an HPLC assay was used to determine the encapsulation efficiency of tacrolimus. The average molecular weights of the synthesized copolymers were in the range of 8,400–28,000 with narrow distributions (PDI=1.06–1.11). The copolymers were designated according to the degree of polymerization of ε-caprolactone, namely PEO114-b-PCL30, PEO114-b-PCL60, PEO114-b-PCL120, and PEO114-b-PCL200. All the prepared micelles were having diameters sizes less than 100nm with narrow distributions. The highest drug solubilization was achieved with PEO114-b-PCL120, where the aqueous solubility of tacrolimus exceeded 300μg/mL. Our results show a potential for PEO-b-PCL micelles as solubilizing vehicles for the delivery of tacrolimus.


      PubDate: 2016-07-27T08:51:23Z
       
  • Synthesis and antimicrobial properties of 4-acylaminobenzenethiosulfoacid
           S-esters

    • Abstract: Publication date: Available online 1 July 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Vira Lubenets, Sofiya Vasylyuk, Nataliya Monka, Khrystyna Bolibrukh, Olena Komarovska-Porokhnyavets, Diana Baranovych, Rostyslav Musyanovych, Ewa Zaczynska, Anna Czarny, Urszula Nawrot, Volodymyr Novikov
      A series of esters of 4-acetyl, 4-trifluoroacetyl- and 4-(3-chloropropionyl)aminobenzenethiosulfoacids (twenty-four compounds) were synthesized and characterized by elemental analysis, 1H NMR and IR spectroscopy. The antibacterial activity of the novel candidates has been screened using the agar diffusion or serial dilution methods against representative Gram-positive (Staphylococcus aureus, Bacillus subtilis, Bacillus mesentericus, Mycobacterium sp., Mycobacterium luteum), Gram-negative (Aeromonas sp., Burkholderia cepacia, Alcaligenes faecalis, Pseudomonas aeruginosa, Escherichia coli, Proteus vulgaris) bacteria and fungi (Candida albicans, Candida tenuis, Candida glabrata, Verticillium dahliae, Trichophyton gypseum, Aspergillus niger, Aspergillus fumigatus, Penicillium chrysogenum). Particular potency has been discovered against all tested pathogenic bacteria and fungi by compounds 1l and 3l at nanomolar concentrations. Some appropriate effect of thiosulfoesters structure upon their antimicrobial activity was determined.


      PubDate: 2016-07-27T08:51:23Z
       
  • Synthesis of chalcone incorporated quinazoline derivatives as anticancer
           agents

    • Abstract: Publication date: Available online 24 June 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Sapavat Madhavi, Reddymasu Sreenivasulu, Jyothsna Pragathi Yazala, Rudraraju Ramesh Raju
      A series of ten novel chalcone incorporated quinazoline derivatives (11a–11j) were designed and synthesized. All the synthesized compounds were evaluated for their anticancer activities against four human cancer cell lines (A549, HT-29, MCF-7 and A375). Among them, four compounds, 11f, 11g, 11i and 11j showed more potent anticancer activity than the control drug, Combretastatin – A4.


      PubDate: 2016-07-27T08:51:23Z
       
  • New Microbial Source of the Antifungal Allylamine
           “Terbinafine”

    • Abstract: Publication date: Available online 24 June 2016
      Source:Saudi Pharmaceutical Journal
      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 enable 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: 2016-07-27T08:51:23Z
       
  • Biologically-guided isolation of leishmanicidal secondary metabolites from
           Euphorbia peplus L.

    • Abstract: Publication date: Available online 22 June 2016
      Source:Saudi Pharmaceutical Journal
      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: 2016-07-27T08:51:23Z
       
  • d-α-tocopherol nanoemulsions: Size properties, rheological behavior,
           surface tension, osmolarity and cytotoxicity

    • Abstract: Publication date: Available online 22 June 2016
      Source:Saudi Pharmaceutical Journal
      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: 2016-07-27T08:51:23Z
       
  • Antiproliferative and apoptotic effect of Morus nigra extract on human
           prostate cancer cells

    • Abstract: Publication date: Available online 20 June 2016
      Source:Saudi Pharmaceutical Journal
      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: 2016-07-27T08:51:23Z
       
  • The genetic profiles of CYP1A1, CYP1A2 and CYP2E1 enzymes as
           susceptibility factor in xenobiotic toxicity in Turkish population

    • Abstract: Publication date: Available online 16 June 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Merve Arici, Gül Özhan
      Evaluation and sequencing of heritable alterations in the human genome and the large-scale identification of gene polymorphism for understanding the genetic background of individuals in response to potential toxicants are provided by toxicogenetics. Cytochrome P450 (CYP) enzymes play role not only phase I-dependent metabolism of xenobiotics but also metabolism of endogenous compounds. CYP1A1, CYP1A2 and CYP2E1 enzymes, which are in phase I enzymes, are responsible for metabolic activation and detoxification of several chemical compounds. In the present study, it was determined the genotype and allele frequency of CYP1A1∗2A, CYP1A2∗1C, CYP1A2∗1F, CYP2E1 and CYP2E1∗6, very common and functional single-nucleotide polymorphisms (SNPs), in Turkish healthy volunteers. It is believed that the determination of polymorphisms in the enzymes may be beneficial to prevent and reduce and adverse effects and death in response to drugs. The allele frequencies of these genes were 24%, 9%, 33%, 42%, and 12%, respectively. In the present study, the genotype profile of Turkish population was determined about critical enzymes for xenobiotic metabolism. It is suggested that the obtained results might be beneficial in order to dose adjustment of drugs and prevention of adverse reactions, and further investigation about mentioned enzymes and their polymorphisms.


      PubDate: 2016-07-27T08:51:23Z
       
  • Prolonged exposure of colon cancer cells to 5-fluorouracil nanoparticles
           improves its anticancer activity

    • Abstract: Publication date: Available online 6 June 2016
      Source:Saudi Pharmaceutical Journal
      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: 2016-07-27T08:51:23Z
       
  • Synthesis and evaluation of anticancer activity of 6-pyrazolinylcoumarin
           derivatives

    • Abstract: Publication date: Available online 3 June 2016
      Source:Saudi Pharmaceutical Journal
      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: 2016-07-27T08:51:23Z
       
  • Prevalence of UDP-glucuronosyltransferase polymorphisms (UGT1A6∗2,
           1A7∗12, 1A8∗3, 1A9∗3, 2B7∗2, and 2B15∗2) in
           a Saudi population

    • Abstract: Publication date: Available online 2 June 2016
      Source:Saudi Pharmaceutical Journal
      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: 2016-07-27T08:51:23Z
       
  • 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

    • Abstract: Publication date: Available online 26 May 2016
      Source:Saudi Pharmaceutical Journal
      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: 2016-07-27T08:51:23Z
       
  • Chitosan treatment abrogates hypercholesterolemia-induced
           erythrocyte’s arginase activation

    • Abstract: Publication date: Available online 26 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Gamaleldin I. Harisa, Sabry M. Attia, Khairy M.A. Zoheir, Fars K. Alanazi
      This study aimed to evaluate the protective effect of chitosan (CS) against hypercholesterolemia (HC) induced arginase activation and disruption of nitric oxide (NO) biosynthesis using erythrocytes as cellular model. Human erythrocytes were isolated and classified into eight groups. Next, cells were treated with l-arginine (l-ARG), Nω-nitro-l-arginine methyl ester (l-NAME), CS or CS+ l-ARG in the presence of normal plasma or cholesterol enriches plasma. Then, erythrocytes were incubated at 37°C for 24h. The present results revealed that, HC induced significant increase of cholesterol inclusion into erythrocytes membrane compared to control. Moreover, HC caused significant decrease in nitric oxide synthase (NOS) activity similar to l-NAME; however, arginase activity and arginase/NOS ratio significantly increased compared to control. On contrast, treatment of HC with, l-arginine, CS or CS plus l-arginine prevents HC induced cholesterol loading into erythrocytes membrane, NOS inhibition and arginase activation. This study suggested that CS could be protective agent against HC induced disruption of erythrocyte’s oxidative status and arginase activation.


      PubDate: 2016-07-27T08:51:23Z
       
  • Development and validation of bioanalytical UHPLC-UV method for
           simultaneous analysis of unchanged fenofibrate and its metabolite
           fenofibric acid in rat plasma: Application to pharmacokinetics

    • Abstract: Publication date: Available online 26 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Rayan G. Alamri, Kazi Mohsin, Ajaz Ahmad, Mohammad Raish, Fars K. Alanazi
      A simple, precise, selective and fast ultra-high performance liquid chromatography (UHPLC-UV) method has been developed and validated for the simultaneous determination of a lipid regulating agent fenofibrate and its metabolite fenofibric acid in rat plasma. The chromatographic separation was carried out on a reversed-phase Acquity® BEH C18 column using methanol–water (65:35, v/v) as the mobile phase. The isocratic flow was 0.3ml/min with rapid run time of 2.5min and UV detection was at 284nm. The method was validated over a concentration range of 100–10000ng/ml (r 2 ⩾0.9993). The selectivity, specificity, recovery, accuracy and precision were validated for determination of fenofibrate/fenofibric acid in rat plasma. The lower limits of detection and quantitation of the method were 30 and 90ng/ml for fenofibrate and 40 and 100ng/ml for fenofibric acid, respectively. The within and between-day coefficients of variation were less than 5%. The validated method has been successfully applied to measure the plasma concentrations in pharmacokinetics study of fenofibrate in an animal model to illustrate the scope and application of the method.


      PubDate: 2016-07-27T08:51:23Z
       
  • New acyclic secondary metabolites from the biologically active fraction of
           Albizia lebbeck flowers

    • Abstract: Publication date: Available online 24 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Shaza M. Al-Massarani, Ali A. El Gamal, Mohamed F. Abd El Halim, Mansour S. Al-Said, Maged S. Abdel-Kader, Omer A. Basudan, Saleh I. Alqasoumi
      The total extract of Albizia lebbeck flowers was examined in vivo for its possible hepatoprotective activity in comparison with the standard drug silymarin at two doses. The higher dose expressed promising activity especially in reducing the levels of AST, ALT and bilirubin. Fractionation via liquid–liquid partition and reexamination of the fractions revealed that the n-butanol fraction was the best in improving liver biochemical parameters followed by the n-hexane fraction. However, serum lipid parameters were best improved with CHCl3 fraction. The promising biological activity results initiated an intensive chromatographic purification of A. lebbeck flowers fractions. Two compounds were identified from natural source for the first time, the acyclic farnesyl sesquiterpene glycoside1-O-[6-O-α-l-arabinopyranosyl-β-d-glucopyranoside]-(2E,6E-)-farnesol (6) and the squalene derivative 2,3-dihydroxy-2,3-dihydrosqualene (9), in addition to eight compounds reported here for the first time from the genus Albizia; two benzyl glycosides, benzyl 1-O-β-d-glucopyranoside (1) and benzyl 6-O-α-l-arabinopyranosyl β-d-glucopyranoside (2); three acyclic monoterpene glycosides, linalyl β-d-glucopyranoside (3) and linalyl 6-O-α-l-arabinopyranosyl-β-d-glucopyranoside (4); (2E)-3,7-dimethylocta-2,6-dienoate-6-O-α-l arabinopyranosyl-β-d-glucopyranoside (5), two oligoglycosides, n-hexyl-α-l arabinopyranosyl-(1→6)-β-d-glucopyranoside (creoside) (7) and n-octyl α-l-arabinopyranosyl-(1→6)-β-d-glucopyranoside (rhodiooctanoside) (8); and ethyl fructofuranoside (10). The structures of the isolated compounds were elucidated based on extensive examination of their spectroscopic 1D and 2D-NMR, MS, UV, and IR data. It is worth mentioning that, some of the isolated linalol glycoside derivatives were reported as aroma precursors.


      PubDate: 2016-07-27T08:51:23Z
       
  • Bioactivity and chemical characterization of Acalypha fruticosa Forssk.
           growing in Saudi Arabia

    • Abstract: Publication date: Available online 24 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Ghada Ahmed Fawzy, Areej Mohammad Al-Taweel, Shagufta Perveen, Shabana Iqrar Khan, Fatma Abdulaziz Al-Omary
      Acalypha is an important genus of the Euphorbiaceae family. The genus is represented by five species in Saudi Arabia. Acalypha fruticosa Forssk. Fl. Aeg is traditionally used as a cure for stomachache, dyspepsia, rheumatism, dermatitis, and swellings of the body. The present study endeavors to provide a phytochemical and biological evaluation of the plant, with the aim of relating activity to constituting secondary metabolites in the plant. Column chromatographic separation of the methanol extract led to the isolation of four compounds namely 2-methyl-5,7-dihydroxychromone 5-O-β-d-glucopyranoside 1, acalyphin 2, apigenin 3 and kaempferol 3-O-rutinoside 4. The plant extracts and the isolated compounds were subjected to biological assays to screen peroxisome proliferator-activated receptor alpha (PPARα) and PPARγ agonistic, anti-inflammatory and cytotoxic activities. Results proved for the first time, the PPARγ activator effect of acalyphin, as well as its promising anti-inflammatory activity, in addition to the dual PPAR activator effect of the chromone glucoside. The plant extracts and isolated compounds were non-cytotoxic to the tested cell lines. Thus A. fruticosa could be a valuable source of important therapeutics that may hold clinical prospect.


      PubDate: 2016-07-27T08:51:23Z
       
  • Compatibility study of paracetamol, chlorpheniramine maleate and
           phenylephrine hydrochloride in physical mixtures

    • Abstract: Publication date: Available online 7 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): G.G.G. de Oliveira, A. Feitosa, K. Loureiro, A.R. Fernandes, E.B. Souto, P. Severino
      Paracetamol (PAR), phenylephrine hydrochloride (PHE) and chlorpheniramine maleate (CPM) are commonly used in clinical practice as antipyretic and analgesic drugs to ameliorate pain and fever in cold and flu conditions. The present work describes the use of thermal analysis for the characterization of the physicochemical compatibility between drugs and excipients during the development of solid dosage forms. Thermogravimetric analysis (TGA) and Differential Scanning Calorimetry (DSC) were used to study the thermal stability of the drug and of the physical mixture (drug/excipients) in solid binary mixtures (1:1). DSC thermograms demonstrated reproducible melting event of the prepared physical mixture. Starch, mannitol, lactose and magnesium stearate influence thermal parameters. Information recorded from the derivative thermogravimetric (DTG) and TGA curves demonstrated the decomposition of drugs in well-defined thermal events, translating the suitability of these techniques for the characterization of the drug/excipients interactions.


      PubDate: 2016-07-27T08:51:23Z
       
  • Acute toxicity profiling of the ethyl acetate fraction of Swietenia
           macrophylla seeds and in-vitro neuroprotection studies

    • Abstract: Publication date: Available online 7 May 2016
      Source:Saudi Pharmaceutical Journal
      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: 2016-07-27T08:51:23Z
       
  • Histatin peptides: Pharmacological functions and their applications in
           dentistry

    • Abstract: Publication date: Available online 4 May 2016
      Source:Saudi Pharmaceutical Journal
      Author(s): Zohaib Khurshid, Shariq Najeeb, Maria Mali, Syed Faraz Moin, Syed Qasim Raza, Sana Zohaib, Farshid Sefat, Muhammad Sohail Zafar
      There are many human oral antimicrobial peptides responsible for playing important roles including maintenance, repairing of oral tissues (hard or soft) and defense against oral microbes. In this review we have highlighted the biochemistry, physiology and proteomics of human oral histatin peptides, secreted from parotid and submandibular salivary glands in human. The significance of these peptides includes capability for ionic binding that can kill fungal Candida albicans. They have histidine rich amino acid sequences (7–12 family members; corresponding to residues 12–24, 13–24, 12–25, 13–25, 5–11, and 5–12, respectively) for Histatin-3. However, Histatin-3 can be synthesized proteolytically from histatin 5 or 6. Due to their fungicidal response and high biocompatibility (little or no toxicity), these peptides can be considered as therapeutic agents with most probable applications for example, artificial saliva for denture wearers and salivary gland dysfunction conditions. The objectives of current article are to explore the human histatin peptides for its types, chemical and biological aspects. In addition, the potential for therapeutic bio-dental applications has been elaborated.


      PubDate: 2016-07-27T08:51:23Z
       
  • Editorial Board

    • Abstract: Publication date: May 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 3




      PubDate: 2016-07-27T08:51:23Z
       
  • Natural cures for breast cancer treatment

    • Abstract: Publication date: May 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 3
      Author(s): Munazza Shareef, Muhammad Aqeel Ashraf, Maliha Sarfraz
      For centuries, herbs and plants have been used for medicinal purposes and as food as well. This review concerns about different types of plants that retain the immune stimulating and anti-tumor properties. Large variety of active phytochemicals such as carotenoids, flavonoids, ligands, polyphenolics, terpenoids, sulfides, lignans and plant sterols has been identified in different types of herbs. These phytochemicals have different mechanisms of action. They either stimulate the protective enzyme like glutathione transferase or prevent the cell proliferation. This review has centered on the biochemical properties of Allium sativum, Echinacea, Curcuma longa, Arctium lappa, Camellia sinensis, Panax ginseng and Flax seed. Extracts and juices of Withania somnifera, Amoora rohituka, Dysoxylum binectariferum and Vaccinium macrocarpon, respectively also used as anti-breast cancer. The volatile oils and extracts of these herbs and plants inhibit the synthesis of mevalonate that lessen the tumor growth and cholesterol synthesis.


      PubDate: 2016-07-27T08:51:23Z
       
  • Separation and purification and in vitro anti-proliferative activity of
           leukemia cell K562 of Galium aparine L. petroleum ether phase

    • Abstract: Publication date: May 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 3
      Author(s): Guoqing Shi, Jiang Liu, Wen’en Zhao, Yanqi Liu, Xinfeng Tian
      To explore material basis of in vitro anti-proliferative activity of leukemia cell K562 of petroleum ether phase of product resulting from Galium aparine L. 60% ethanol extraction, the experiment adopts column chromatography combined with thin layer preparation, isolates and purifies petroleum ether, conducts structural identification of obtained single compound and applies MTT method for viability assay of in vitro anti-proliferative activity of leukemia cell K562. Experimental results show that G. aparine L. petroleum ether contains mainly β-sitosterol, daucosterol and dibutyl phthalate and other substances. Under experimental conditions, the three could inhibit the proliferation of leukemia cell K562 with dose-effect and time-effect relationship, of which dibutyl phthalate has strongest activity. Dibutyl phthalate with excellent activity, β-sitosterol with rich content and moderate effect should be the main contributor to its biological activity.


      PubDate: 2016-07-27T08:51:23Z
       
  • Release property study on the novel divalproex sodium enteric-coated
           capsules

    • Abstract: Publication date: May 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 3
      Author(s): Shuoye Yang, Xin Wang, Jiangsong Jia, Pengyuan Li
      In the present study, a novel divalproex sodium (DS) enteric-coated capsule was prepared, and high performance liquid chromatography (HPLC) assay method for DS was developed. Their uniformity, release curve and release characteristics in different solvents were examined. The release studies were performed using marketed sample as a reference and data were analyzed in terms of cumulative release amounts as a function of time. It was demonstrated by the results that assay developed was specific, rapid and reliable, which can be used to determine DS in vitro accurately, and our developed samples were similar to reference preparation in in vitro release characteristics. The release characteristics of different batches of samples were quite similar to each other, and the total release percents of DS from enteric-coated capsule were within 0–10% in HCl, and reached close to 100% in phosphate buffer. Similarity factors (f 2) of three batches between two preparations were all higher than 50. The developed enteric-coated capsule may be a promising alternative dosage form for treatment of related diseases.


      PubDate: 2016-07-27T08:51:23Z
       
  • Study on fluorouracil–chitosan nanoparticle preparation and its
           antitumor effect

    • Abstract: Publication date: May 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 3
      Author(s): Gaimin Chen, Rudong Gong
      To successfully prepare fluorouracil–chitosan nanoparticles, and further analyze its anti-tumor activity mechanism, this paper makes a comprehensive study of existing preparation prescription and makes a detailed analysis of fluorouracil–chitosan in vitro release and pharmacodynamic behavior of animals. Two-step synthesis method is adopted to prepare 5-FU–CS–mPEG prodrugs, and infrared, 1H NMR and differential thermal analysis are adopted to analyze characterization synthetic products of prepared drugs. To ensure clinical efficacy of prepared drugs, UV spectrophotometry is adopted for determination of drug loading capacity of prepared drugs, transmission electron microscopy is adopted to observe the appearance, dynamic dialysis method is used to observe in vitro drug release of prepared drugs and fitting of various release models is done. Anti-tumor effect is studied via level of animal pharmacodynamics. After the end of the experiment, tumor inhibition rate, spleen index and thymus index of drugs are calculated. Experimental results show that the prepared drugs are qualified in terms of regular shape, dispersion, drug content, etc. Animal pharmacodynamics experiments have shown that concentration level of drug loading capacity of prepared drugs has a direct impact on anti-tumor rate. The higher the concentration, the higher the anti-tumor rate. Results of pathological tissue sections of mice show that the prepared drugs cause varying degrees of damage to receptor cells, resulting in cell necrosis or apoptosis problem. It can thus be concluded that ion gel method is an effective method to prepare drug-loading nanoparticles, with prepared nanoparticles evenly distributed in regular shape which demonstrate good slow-release characteristics in receptor vitro and vivo. At the same time, after completion of drug preparation, relatively strong anti-tumor activity can be generated for the receptor, so this mode of preparation enjoys broad prospects for development.


      PubDate: 2016-07-27T08:51:23Z
       
  • Preparation and application of functionalized nano drug carriers

    • Abstract: Publication date: May 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 3
      Author(s): Rudong Gong, Gaimin Chen
      Objective: Targeting at category memory characteristics and preparation methods of functionalized nano drugs, preparation technology of functionalized nano drug carriers is studied, and then important role of functionalized nano drug carrier in preparation of medicine is studied. Methods: Carry out the relevant literature search with computer, change limited language in the paper to Chinese and necessarily remove repetitive studies. Results: After first review of 1260 retrieved literature, it can be found that nano drug is with accurate quantity, relatively good targeting, specificity and absorbency. Necessary research of nano drug carriers can prevent and treat disease to a certain extent. Conclusion: Preparation of functionalized nanocarrier is simple and convenient, which can improve frequency of use of nano preparation technology and provide better development space for medical use. Therefore, nanocarriers should be combined with drugs with relatively strong specificity in clinics, in order to be able to conduct effective research on nanometer intelligent drug, effectively promote long-term development of nano biotechnology, and then provide favorable, reliable basis for clinical diagnosis and treatment.


      PubDate: 2016-07-27T08:51:23Z
       
  • Forgotten topological index of chemical structure in drugs

    • Abstract: Publication date: May 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 3
      Author(s): Wei Gao, Muhammad Kamran Siddiqui, Muhammad Imran, Muhammad Kamran Jamil, Mohammad Reza Farahani
      A massive of early drug tests implies that there exist strong inner relationships between the bio-medical and pharmacology characteristics of drugs and their molecular structures. The forgotten topological index was defined to be used in the analysis of drug molecular structures, which is quite helpful for pharmaceutical and medical scientists to grasp the biological and chemical characteristics of new drugs. Such tricks are popularly employed in developing countries where enough money is lacked to afford the relevant chemical reagents and equipment. In our article, by means of drug molecular structure analysis and edge dividing technology, we present the forgotten topological index of several widely used chemical structures which often appear in drug molecular graphs.


      PubDate: 2016-07-27T08:51:23Z
       
  • Diagnosis of Genus Helicobacter through a hemi-nested PCR assay of 16S
           rRNA

    • Abstract: Publication date: May 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 3
      Author(s): Heping Qin, Guodu Tang, Ping Yi, Xinyi Pan, Huali Huang, Renjie Chang, Zhe Shi, Muhammad Aqeel Ashraf
      The present study aimed to establish a genus-specific PCR-based assay to detect helicobacters using 16S rRNA gene as the target template. We designed the hemi-nested primers based on sequences of 16S rRNA gene of 34 types of Helicobacter species. The inclusivity, sensitivity, and specificity of the PCR assay using these primers were examined in three different models, comprising feces simulated samples, BLAB/c mice infection model and clinic patients samples. The detection sensitivity of Helicobacter pylori, Helicobacter hepaticus and Helicobacter bilis strains from feces simulated samples was all 102CFU/ml. We successfully detected H. hepaticus and H. bilis in the liver, cecum and feces of experimentally infected mice. H. pylori was successfully detected in the feces samples from 3 patients infected with H. pylori while not in the feces samples from 3 healthy human. However, the C97/C05–C97/C98 PCR assay detected H. pylori in the 2 positive samples. Due to the PCR assay’s excellent inclusivity, high sensitivity and specificity it may be used to detect the presence of Helicobacters.


      PubDate: 2016-07-27T08:51:23Z
       
  • Endophytic filamentous fungi from a Catharanthus roseus: Identification
           and its hydrolytic enzymes

    • Abstract: Publication date: May 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 3
      Author(s): Farah Wahida Ayob, Khanom Simarani
      This paper reported on the various filamentous fungi strains that were isolated from a wild grown Catharanthus roseus. Based on the morphological characteristics and molecular technique through a Polymerase Chain Reaction and DNA sequencing method using internal transcribed spacer (ITS), these fungi had been identified as a Colletotrichum sp., Macrophomina phaseolina, Nigrospora sphaerica and Fusarium solani. The ultrastructures of spores and hyphae were observed under a Scanning Electron Microscope. The hydrolytic enzyme test showed that all strains were positive in secreting cellulase. Colletotrichum sp. and F. solani strains also gave a positive result for amylase while only F. solani was capable to secrete protease. These fungi were putatively classified as endophytic fungi since they produced extracellular enzymes that allow them to penetrate plant cell walls and colonize with symbiotic properties.


      PubDate: 2016-07-27T08:51:23Z
       
  • New discovery of cryptorchidism: Decreased retinoic acid in testicle

    • Abstract: Publication date: May 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 3
      Author(s): Jinpu Peng, Lianju Shen, Jinjun Chen, Xining Cao, Yue Zhou, Huali Weng, Chunlan Long, Deying Zhang, Shengfen Tu, Yan Zhang, Dawei He, Tao Lin, Guanghui Wei
      This study focuses on investigation of cryptorchidism induced by flutamide (Flu) and its histopathological damage, and detects retinoic acid concentration in testicle tissue, in order to find a new method for clinical treatment to infertility caused by cryptorchidism. Twenty SD (Sprague Dawley) pregnant rats were randomly divided into Flu cryptorchidism group (n =10) and normal control group (n =10). HE stained for observing morphological difference. Transmission electron microscope (TEM) was used for observing the tight junction structure between Sertoli cells. Epididymal caudal sperms were counted and observed in morphology. The expression of stimulated by retinoic acid gene 8 (Stra8) was detected using immunohistochemistry, western blot, and Q-PCR. High performance liquid chromatography (HPLC) analysis was made on retinoic acid content. Sperm count and morphology observation confirmed cryptorchidism group was lower than normal group in sperm quantity and quality. The observation by TEM showed a loose structure of tight junctions between Sertoli cells. Immunohistochemistry, western blot, and Q-PCR showed that cryptorchidism group was significantly lower than normal group in the expression of Stra8. HPLC showed that retinoic acid content was significantly lower in cryptorchid testis than in normal testis. In the cryptorchidism model, retinoic acid content in testicular tissue has a significant reduction; testicles have significant pathological changes; damage exists in the structure of tight junctions between Sertoli cells; Stra8 expression has a significant reduction, perhaps mainly contributing to spermatogenesis disorder.


      PubDate: 2016-07-27T08:51:23Z
       
  • The transport mechanism of monocarboxylate transporter on spinosin in
           Caco-2 cells

    • Abstract: Publication date: May 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 3
      Author(s): Xiang Le Meng, Yan Li Guo, Hai Ying Huang
      Objectives: The aim of this study was to determine the uptake mechanism of spinosin (SPI) by the monocarboxylic acid transporters (MCTs) in Caco-2 cells. Methods: The Caco-2 cells were pretreated with various monocarboxylic acids, and the uptake of spinosin from Caco-2 cells was measured by High Performance Liquid Chromatography (HPLC). Key findings: Preloading of various monocarboxylic acids enhanced the uptake of SPI, especially salicylic acid (a substrate of MCTs) had a 23.4 times increase in SPI uptake, indicating that the monocarboxylic acid transporters had an efflux effect on SPI uptake and salicylic acid had a strong inhibition on SPI efflux in Caco-2 cells. At the same time, the uptake of SPI through Caco-2 cells was Na+- and temperature-dependent, pretreatment without Na+ significantly increased the uptake of SPI by 1.85 times and incubated at low temperature (4°C) SPI uptake increased 20% than that of 37°C. Furthermore, SPI was transported mainly via a carrier-mediated transport: [Vmax=5.364μg/mg protein, Km=657.0μg/mL]. Conclusion: The uptake of spinosin (SPI) in Caco-2 cells was mainly regulated by the monocarboxylic acid transporters along with Salicylic acid.


      PubDate: 2016-07-27T08:51:23Z
       
  • The effect of chitooligosaccharides on oleic acid-induced lipid
           accumulation in HepG2 cells

    • Abstract: Publication date: May 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 3
      Author(s): Peiqiu Cao, Guidong Huang, Qingyun Yang, Jiao Guo, Zhengquan Su
      This experiment aimed to evaluate the capacities of two types of chitooligosaccharides (COS) with different molecular weights for the ability to eliminate lipid accumulation in hepatocytes. We have established a lipid accumulation model in HepG2 cells for these studies in vitro, which was established by induction with oleic acid. The capacity of COS to eliminate lipid accumulation was evaluated using three metrics: the thiazolyl blue dye absorbance (MTT value), the morphology of intracellular lipid droplets and the triglyceride level (TG). Two types of COS with different molecular weights (1000Da and 3000Da) can significantly reduce intracellular lipid accumulation and decrease TG content in HepG2 cells, in a dose-dependent fashion. We found that low molecular weight COS is more efficacious than high molecular weight COS. Two types of COS can eliminate lipid accumulation induced by oleic acid in HepG2 cells, leading to an obvious hypolipidemic effect in vitro. These results suggest that COS may be effective preventive agents in fatty liver disease.


      PubDate: 2016-07-27T08:51:23Z
       
  • Patients treatment with neuroglioma by teniposide and semustine and its
           influence on Twist and E-cadherin expression

    • Abstract: Publication date: May 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 3
      Author(s): Yongbo Zhang, Guoyi Liu, Meiling Lang, Jing Zhang, Jia Geng
      This study focuses on curative effects of teniposide combining with semustine on patients with neuroglioma and the influences on the expression of Twist and E-cadherin in tissue. Sixty-eight patients with neuroglioma taking operation in our hospital were divided into two groups randomly. Single radiotherapy was given to 34 patients in group A, and teniposide (VM-26) and semustine (Me-CCUN) were added to radiotherapy for 34 patients in group B. Then, curative effects, survival rate, living quality and adverse reaction rate after operation were compared between two groups. Moreover, the difference in positive expression rate of Twist and E-cadherin before and after treatment between two groups was analyzed by immunohistochemistry. Results: In group B, the effective rate of treatment was 88.2%, and the disease control rate was 70.6%, higher than 52.9% and 32.4% in group A with statistical significance (P <0.05). Moreover, the survival rate in three years of group B was 44.1%, and the score of living quality was 67.11±4.32, and also higher than 23.5% and 63.79±4.53 in group A with statistical significance (P <0.05). However, the difference between two groups in adverse reaction rate has no statistical significance (P >0.05). In addition, the difference in positive expression rate of Twist and E-cadherin between group A and group B has no statistical significance before treatment (P >0.05). After treatment, however, the positive rate of Twist in group B is lower than that in group A, while the positive rate of E-cadherin is higher. Both differences have statistical significance (P <0.05). Chemotherapy of VM-26 combining with Me-CCNU can inhibit Twist expression and improve the expression rate of E-cadherin to help improving the curative effects and living quality and increasing survival rate.


      PubDate: 2016-07-27T08:51:23Z
       
  • Biomechanical analysis of press-extension technique on degenerative lumbar
           with disc herniation and staggered facet joint

    • Abstract: Publication date: May 2016
      Source:Saudi Pharmaceutical Journal, Volume 24, Issue 3
      Author(s): Hong-gen Du, Sheng-hui Liao, Zhong Jiang, Huan-ming Huang, Xi-tao Ning, Neng-yi Jiang, Jian-wei Pei, Qin Huang, Hui Wei
      This study investigates the effect of a new Chinese massage technique named “press-extension” on degenerative lumbar with disc herniation and facet joint dislocation, and provides a biomechanical explanation of this massage technique. Self-developed biomechanical software was used to establish a normal L1–S1 lumbar 3D FE model, which integrated the spine CT and MRI data-based anatomical structure. Then graphic technique is utilized to build a degenerative lumbar FE model with disc herniation and facet joint dislocation. According to the actual press-extension experiments, mechanic parameters are collected to set boundary condition for FE analysis. The result demonstrated that press-extension techniques bring the annuli fibrosi obvious induction effect, making the central nucleus pulposus forward close, increasing the pressure in front part. Study concludes that finite element modelling for lumbar spine is suitable for the analysis of press-extension technique impact on lumbar intervertebral disc biomechanics, to provide the basis for the disease mechanism of intervertebral disc herniation using press-extension technique.


      PubDate: 2016-07-27T08:51:23Z
       
 
 
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