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  Subjects -> PHARMACY AND PHARMACOLOGY (Total: 575 journals)
Showing 401 - 253 of 253 Journals sorted alphabetically
Microbial Drug Resistance     Hybrid Journal   (Followers: 3)
Molecular Informatics     Hybrid Journal   (Followers: 5)
Molecular Pharmacology     Hybrid Journal   (Followers: 2)
Molekul     Open Access   (Followers: 1)
Natural Product Communications     Open Access  
Nature Reviews Drug Discovery     Full-text available via subscription   (Followers: 313)
Naunyn-Schmiedeberg's Archives of Pharmacology     Hybrid Journal  
NeuroMolecular Medicine     Hybrid Journal  
Neuropharmacology     Hybrid Journal   (Followers: 5)
Neuropsychopharmacology     Hybrid Journal   (Followers: 17)
Neuropsychopharmacology Reports     Open Access  
Nigerian Journal of Natural Products and Medicine     Full-text available via subscription  
OA Drug Design & Delivery     Open Access  
OA Medical Hypothesis     Open Access  
Obesity Facts     Open Access   (Followers: 8)
Open Pharmacoeconomics & Health Economics Journal     Open Access   (Followers: 1)
Open Pharmacology Journal     Open Access  
OpenNano     Open Access   (Followers: 1)
Orbital - The Electronic Journal of Chemistry     Open Access   (Followers: 1)
Oriental Pharmacy and Experimental Medicine     Partially Free   (Followers: 2)
Pain and Therapy     Open Access   (Followers: 3)
Particulate Science and Technology: An International Journal     Hybrid Journal   (Followers: 1)
PDA Journal of Pharmaceutical Science and Technology     Full-text available via subscription   (Followers: 34)
Pediatric Drugs     Full-text available via subscription   (Followers: 3)
Pediatric Pharmacology     Open Access   (Followers: 1)
Pharmaceutica Analytica Acta     Open Access  
Pharmaceutical Biology     Open Access  
Pharmaceutical Care-La Farmacoterapia     Open Access  
Pharmaceutical Chemistry Journal     Hybrid Journal  
Pharmaceutical Development and Technology     Hybrid Journal   (Followers: 19)
Pharmaceutical Executive     Full-text available via subscription   (Followers: 2)
Pharmaceutical Fronts     Open Access   (Followers: 9)
Pharmaceutical Historian     Open Access  
Pharmaceutical Journal     Free   (Followers: 8)
Pharmaceutical Journal of Sri Lanka     Open Access  
Pharmaceutical Medicine     Full-text available via subscription   (Followers: 4)
Pharmaceutical Nanotechnology     Hybrid Journal  
Pharmaceutical Patent Analyst     Full-text available via subscription   (Followers: 3)
Pharmaceutical Research     Hybrid Journal   (Followers: 93)
Pharmaceutical Statistics     Hybrid Journal   (Followers: 15)
Pharmaceutical Technology     Full-text available via subscription   (Followers: 7)
Pharmaceuticals     Open Access   (Followers: 4)
Pharmacia     Open Access  
Pharmaciana     Open Access  
PharmacoEconomics     Full-text available via subscription   (Followers: 25)
PharmacoEconomics & Outcomes News     Full-text available via subscription   (Followers: 2)
PharmacoEconomics German Research Articles     Full-text available via subscription  
PharmacoEconomics Spanish Research Articles     Hybrid Journal   (Followers: 1)
Pharmacoepidemiology and Drug Safety     Hybrid Journal   (Followers: 33)
Pharmacogenetics and Genomics     Hybrid Journal   (Followers: 1)
Pharmacogenomics     Hybrid Journal   (Followers: 7)
Pharmacogenomics and Personalized Medicine     Open Access   (Followers: 2)
Pharmacogenomics Journal     Hybrid Journal   (Followers: 5)
Pharmacognosy Communications     Partially Free  
Pharmacognosy Magazine     Open Access   (Followers: 2)
Pharmacognosy Research     Open Access   (Followers: 2)
Pharmacological Reports     Hybrid Journal  
Pharmacological Research     Hybrid Journal   (Followers: 1)
Pharmacological Research - Modern Chinese Medicine     Open Access  
Pharmacological Reviews     Hybrid Journal   (Followers: 2)
Pharmacology     Full-text available via subscription  
Pharmacology & Therapeutics     Hybrid Journal   (Followers: 3)
Pharmacology & Pharmacy     Open Access   (Followers: 1)
Pharmacology Biochemistry and Behavior     Hybrid Journal   (Followers: 2)
Pharmacology Research & Perspectives     Open Access  
Pharmacon : Jurnal Farmasi Indonesia     Open Access  
Pharmacopsychiatry     Hybrid Journal   (Followers: 3)
Pharmacotherapy The Journal of Human Pharmacology and Drug Therapy     Hybrid Journal   (Followers: 37)
Pharmactuel     Open Access   (Followers: 1)
Pharmacy     Open Access   (Followers: 4)
Pharmacy & Pharmacology     Open Access   (Followers: 1)
Pharmacy Education     Full-text available via subscription   (Followers: 11)
Pharmacy Practice (Internet)     Open Access   (Followers: 8)
Pharmakon : Arzneimittel in Wissenschaft und Praxis     Full-text available via subscription   (Followers: 1)
PharmaNutrition     Hybrid Journal   (Followers: 3)
PharmaTutor     Open Access  
Pharmazeutische Industrie     Full-text available via subscription   (Followers: 9)
Pharmazeutische Zeitung     Full-text available via subscription   (Followers: 11)
Pharmazie in Unserer Zeit (Pharmuz)     Hybrid Journal   (Followers: 11)
Physiology International     Full-text available via subscription   (Followers: 3)
Plant Products Research Journal     Full-text available via subscription  
Planta Medica     Hybrid Journal   (Followers: 4)
Planta Medica International Open     Open Access  
Prescriber     Hybrid Journal   (Followers: 9)
Progress in Neuro-Psychopharmacology and Biological Psychiatry     Hybrid Journal   (Followers: 8)
Psychiatry and Clinical Psychopharmacology     Open Access   (Followers: 1)
Psychopharmacology     Hybrid Journal   (Followers: 15)
Pulmonary Pharmacology & Therapeutics     Hybrid Journal   (Followers: 2)
PZ Prisma : Materialien zur Fort- und Weiterbildung     Full-text available via subscription  
Redox Report     Open Access  
Regulatory Mechanisms in Biosystems     Open Access   (Followers: 1)
Regulatory Toxicology and Pharmacology     Hybrid Journal   (Followers: 41)
Research & Reviews : A Journal of Drug Design & Discovery     Full-text available via subscription  
Research & Reviews : A Journal of Pharmaceutical Science     Full-text available via subscription  
Research & Reviews : A Journal of Pharmacognosy     Full-text available via subscription  
Research & Reviews : A Journal of Pharmacology     Full-text available via subscription   (Followers: 1)
Research in Pharmaceutical Sciences     Open Access   (Followers: 3)
Research in Social and Administrative Pharmacy     Hybrid Journal   (Followers: 3)
Research Journal of Pharmacognosy     Open Access  
Research Results in Pharmacology     Open Access  
Reviews of Physiology, Biochemistry and Pharmacology     Hybrid Journal   (Followers: 4)
Reviews on Clinical Pharmacology and Drug Therapy     Full-text available via subscription  
Revista Colombiana de Ciencias Químico-Farmacéuticas     Open Access  
Revista Cubana de Plantas Medicinales     Open Access   (Followers: 1)
Revista de Ciências Farmacêuticas Básica e Aplicada     Open Access  
Revista Mexicana de Ciencias Farmaceuticas     Open Access  
Revue de Médecine et de Pharmacie     Full-text available via subscription  
Safety and Risk of Pharmacotherapy     Open Access   (Followers: 1)
Saudi Pharmaceutical Journal     Open Access  
Scandinavian Journal of Clinical and Laboratory Investigation     Hybrid Journal   (Followers: 7)
Scientia Pharmaceutica     Open Access  
Seminars in Hematology     Hybrid Journal   (Followers: 12)
Seminars in Oncology Nursing     Full-text available via subscription   (Followers: 10)
Separation Science plus (SSC plus)     Hybrid Journal  
Side Effects of Drugs Annual     Full-text available via subscription   (Followers: 2)
Skin Pharmacology and Physiology     Full-text available via subscription   (Followers: 6)
Substance Abuse : Research and Treatment     Open Access   (Followers: 5)
Suchttherapie     Hybrid Journal   (Followers: 1)
Sustainable Chemistry and Pharmacy     Full-text available via subscription   (Followers: 1)
Synfacts     Hybrid Journal   (Followers: 5)
SynOpen     Open Access  
The Botulinum J.     Hybrid Journal  
The Brown University Psychopharmacology Update     Hybrid Journal   (Followers: 2)
The Medical Letter     Full-text available via subscription   (Followers: 18)
The Pink Sheet     Full-text available via subscription   (Followers: 13)
The Pink Sheet Daily     Full-text available via subscription   (Followers: 4)
Therapeutic Advances in Drug Safety     Open Access   (Followers: 3)
Therapeutic Advances in Psychopharmacology     Open Access   (Followers: 4)
Therapeutic Advances in Vaccines     Hybrid Journal   (Followers: 1)
Therapeutic Drug Monitoring     Hybrid Journal   (Followers: 3)
Therapeutic Innovation & Regulatory Science     Hybrid Journal   (Followers: 7)
Thérapie     Full-text available via subscription   (Followers: 1)
TheScientist     Free   (Followers: 5)
Toxicological & Environmental Chemistry     Hybrid Journal   (Followers: 2)
Toxicological Research     Hybrid Journal  
Toxicological Sciences     Hybrid Journal   (Followers: 11)
Toxicology     Hybrid Journal   (Followers: 18)
Toxicology and Applied Pharmacology     Hybrid Journal   (Followers: 24)
Toxicology and Industrial Health     Hybrid Journal   (Followers: 6)
Toxicology in Vitro     Hybrid Journal   (Followers: 11)
Toxicology International     Full-text available via subscription   (Followers: 5)
Toxicology Letters     Hybrid Journal   (Followers: 15)
Toxicology Mechanisms and Methods     Hybrid Journal   (Followers: 7)
Toxicology Research     Partially Free   (Followers: 8)
Toxicon     Hybrid Journal   (Followers: 5)
Toxicon : X     Open Access  
Toxin Reviews     Hybrid Journal  
Translational Psychiatry     Open Access   (Followers: 14)
Trends in Peptide and Protein Sciences     Open Access  
Trends in Pharmacological Sciences     Full-text available via subscription   (Followers: 19)
Tropical Journal of Pharmaceutical Research     Open Access  
Ukrainian Biopharmaceutical Journal     Open Access  
Vascular Pharmacology     Hybrid Journal   (Followers: 2)
World Mycotoxin Journal     Hybrid Journal   (Followers: 3)
Yakugaku Zasshi     Open Access   (Followers: 1)
Zeitschrift für Phytotherapie     Hybrid Journal   (Followers: 1)
Актуальні питання фармацевтичної та медичної науки та практики     Open Access  
Фармацевтичний часопис     Open Access  

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Scientia Pharmaceutica
Journal Prestige (SJR): 0.268
Citation Impact (citeScore): 1
Number of Followers: 0  

  This is an Open Access Journal Open Access journal
ISSN (Print) 0036-8709 - ISSN (Online) 2218-0532
Published by MDPI Homepage  [84 journals]
  • Sci. Pharm., Vol. 90, Pages 39: A Narrative Review of the Potential Roles
           of Lipid-Based Vesicles (Vesiculosomes) in Burn Management

    • Authors: Bazigha K. Abdul Rasool, Nema Al Mahri, Nora Alburaimi, Fatima Abdallah, Anfal Saeed Bin Shamma
      First page: 39
      Abstract: Burn injuries can have a lasting effect on people’s quality of life, as they negatively impact their physical and mental health. Then, they are likely to suffer psychological problems as a result. A serious problem is that deep burns are more challenging to treat due to their slow healing rate and susceptibility to microbial infection. Conventional topical medications used for burn treatment are sometimes ineffective because they cannot optimize their ability of transcutaneous absorption at the targeted site and accelerate healing. However, nanotechnology offers excellent prospects for developing current medical wound therapies and is capable of addressing issues such as low drug stability, water solubility, permeability, and bioavailability. The current review focuses on lipid-based vesicles (vesiculosomes) as an example of advanced delivery systems, showing their potential clinical applications in burn wound management. Vesiculosomes may help overcome impediments including the low bioavailability of active agents, offering the controlled release of drugs, increased drug stability, fewer side effects, and reduced dosing frequency, which will ultimately improve therapeutic efficacy and patient compliance. We discuss the application of various types of vesiculosomes such as liposomes, niosomes, ethosomes, cubosomes, transfersomes, and phytosomes in burn healing therapy, as these demonstrate superior skin penetration compared to conventional burn topical treatment. We also highlight their noteworthy uses in the formulation of natural products and discuss the current status as well as future perspectives of these carriers in burn management. Furthermore, the burn treatment options currently available in the market are also summarized.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-06-29
      DOI: 10.3390/scipharm90030039
      Issue No: Vol. 90, No. 3 (2022)
  • Sci. Pharm., Vol. 90, Pages 40: Colorectal Cancer Chemoprevention by
           S-Allyl Cysteine–Caffeic Acid Hybrids: In Vitro Biological Activity
           and In Silico Studies

    • Authors: Angie Herrera-Ramirez, Andres F. Yepes-Pérez, Jorge Quintero-Saumeth, Gustavo Moreno-Quintero, Tonny W. Naranjo, Wilson Cardona-Galeano
      First page: 40
      Abstract: Conventional chemotherapy for colorectal cancer (CRC) gives only a small increase in patient survival, since it is often diagnosed at late stages, when the tumor has disseminated to other organs. Moreover, it is common to observe that malignant cells may acquire resistance to conventional chemotherapies through different mechanisms, including reducing drug activation or accumulation (by enhancing efflux), inducing alterations in molecular targets, and inhibiting the DNA damage response, among other strategies. Considering these facts, the discovery of new molecules with therapeutic potential has become an invaluable tool in chemoprevention. In this context, we previously evaluated two hybrids (SAC-CAFA-MET and SAC-CAFA-PENT) that exhibited selective cytotoxicity against SW480 cells, with better results than the conventional chemotherapeutic agent (5-fluorouracil; 5-FU). Here, we investigated the possible mechanisms of these molecules in greater depth, to identify whether they could be valuable therapeutic scaffolds in the search for new molecules with chemopreventive potential for the treatment of CRC. Both compounds reduced ROS formation, which could be related to antioxidant effects. Further evaluations showed that SAC-CAFA-MET induces cell death independent of caspases and the tumor-suppressor protein p53, but probably mediated by the negative regulation of the pro-apoptotic Bcl-2. In addition, the lack of activation of caspase-8 and the positive regulation of caspase-3 induced by SAC-CAFA-PENT suggest that this compound acts through an apoptotic mechanism, probably initiated by intrinsic pathways. Furthermore, the downregulation of IL-6 by SAC-CAFA-PENT suggests that it also induces a significant anti-inflammatory process. In addition, docking studies would suggest caspase-3 modulation as the primary mechanism by which SAC-CAFA-PENT elicits apoptosis in SW480human colorectal adenocarcinoma cells. Meanwhile, density functional theory (DFT) calculations suggest that both hybrids would produce effects in the modulation of ROS in SW480 cells via the hydrogen atom transfer (HAT) pathway. The present work notes that SAC-CAFA-MET and SAC-CAFA-PENT could be potential candidates for further investigations in the search for potential chemopreventive agents.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-06-30
      DOI: 10.3390/scipharm90030040
      Issue No: Vol. 90, No. 3 (2022)
  • Sci. Pharm., Vol. 90, Pages 41: Emerging Approach for the Application of
           Hibiscus sabdariffa Extract Ointment in the Superficial Burn Care

    • Authors: Rania Khalil, Galal Yahya, Walied S. Abdo, Ghada S. El-Tanbouly, Dina Johar, Mahmoud Saad Abdel-Halim, Hanan Eissa, Calin Magheru, Sameh Saber, Simona Cavalu
      First page: 41
      Abstract: Wound healing comprises organized events involving tissue repair and regeneration. The discovery of toll-like receptors (TLRs) sheds recent light on the mechanisms involved in initiating inflammatory responses throughout the healing cascades. Hibiscus sabdariffa (HS) components may exhibit a wound healing action, owing to their antioxidant and anti-inflammatory activities. This study was designed to investigate the early effects of HS loaded in an ointment base on wound healing, antioxidant, antimicrobial effects, burning intensity, and histopathological features on the rat burn model in comparison to the standard treatment, Iruxol® ointment. A burn injury model was used to evaluate the wound healing potency of the preparation. Rats were treated with ointments three times on the day of the induction of the burn. Findings revealed that the strong antioxidant properties of the HS-loaded ointment augmented the skin healing potential by stimulating biomarkers required for skin regeneration. HS repressed the burning-induced inflammation by the effective reduction in the levels of tumor necrosis factor α (TNF-α) and IL-6 through TLR4 protein inhibition. Topical HS downregulates transforming growth factor-beta (TGF-β) levels. HS extract possesses a potential bactericidal activity against highly resistant clinical isolates of Pseudomonas aeruginosa. Overall, this study proclaims that HS-loaded topical preparations could be a valuable product that serves as adjuvants to accelerate burn wound healing through inactivating the TLR4 pathway.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-06-30
      DOI: 10.3390/scipharm90030041
      Issue No: Vol. 90, No. 3 (2022)
  • Sci. Pharm., Vol. 90, Pages 22: Cinnamaldehyde Relieves Induced
           Hepatocellular Carcinoma in Rat Model via Targeting Wnt/β-Catenin

    • Authors: Al Shaima G. Abd El Salam, Yara A. Samra, Mamdouh M. El-Shishtawy
      First page: 22
      Abstract: Cinnamaldehyde (CA) is a natural compound that has promising biological activity. The current study investigates the antitumor activity of CA in thioacetamide induced hepatocellular carcinoma (HCC) in rats through targeting the Wnt/β-catenin pathway and evaluates the capability of CA to relieve hepatocytes oxidative stress in the HCC-rat model. After 16 weeks of HCC induction by thioacetamide (TAA), rats were treated for 7 consecutive weeks with CA daily; i.p. injection, Alpha-fetoprotein (AFP) level, necroinflammatory score and fibrosis percentage were measured to assess HCC development. The Wnt/β-catenin pathway was evaluated by measuring the hepatic protein level of Wnt-3a, β-catenin, cyclin D, matrix metalloproteinase-9 (MMP-9), and vascular endothelial growth factor (VEGF). Furthermore, hepatocytes’ oxidative stress was assessed by measuring hepatic GSH and MDA contents. Results showed that CA was significantly inhibiting the Wnt/β-catenin pathway through the downregulation of hepatic Wnt-3a, β-catenin, cyclin D, MMP-9, and VEGF. Moreover, CA ameliorates hepatocytes’ oxidative stress via lowering hepatic MDA content and rising hepatic GSH content. Thus, in conclusion, CA is a promising treatment for HCC. It not only has an effective antitumor activity but also ameliorates hepatocytes’ oxidative stress.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-03-31
      DOI: 10.3390/scipharm90020022
      Issue No: Vol. 90, No. 2 (2022)
  • Sci. Pharm., Vol. 90, Pages 23: Enhanced Antibacterial Activity of
           Brevibacillus sp. SPR19 by Atmospheric and Room Temperature Plasma
           Mutagenesis (ARTP)

    • Authors: Nuttapon Songnaka, Mudtorlep Nisoa, Apichart Atipairin, Thamonwan Wanganuttara, Thapanee Chinnawong
      First page: 23
      Abstract: Antibiotic resistance is a major health concern worldwide. In our previous study, some bacterial isolates exhibited antibacterial activity against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA). However, the production of antibacterial substances by native microorganisms is limited by biosynthetic genes. This study aimed to improve the antibacterial activity of SPR19 using atmospheric and room temperature plasma mutagenesis (ARTP). The results showed that SPR19 belonged to the Brevibacillus genus. The growth curves and production kinetics of antibacterial substances were investigated. Argon-based ARTP was applied to SPR19, and the 469 mutants were preliminarily screened using agar overlay method. The remaining 25 mutants were confirmed by agar well diffusion assay against S. aureus TISTR 517 and MRSA isolates 142, 1096, and 2468. M285 exhibited the highest activity compared to the wild-type strain (10.34–13.59%) and this mutant was stable to produce the active substances throughout 15 generations consistently. The antibacterial substances from M285 were tolerant to various conditions (heat, enzyme, surfactant, and pH) while retaining more than 90% of their activities. Therefore, Brevibacillus sp. SPR19 is a potential source of antibacterial substances. ARTP mutagenesis is a powerful method for strain improvement that can be utilized to treat MRSA infection in the future.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-04-06
      DOI: 10.3390/scipharm90020023
      Issue No: Vol. 90, No. 2 (2022)
  • Sci. Pharm., Vol. 90, Pages 24: Repurposing of Four Drugs as
           Anti-SARS-CoV-2 Agents and Their Interactions with Protein Targets

    • Authors: Luis C. Vesga, Camilo A. Ruiz-Hernández, Jeimmy J. Alvarez-Jacome, Jonny E. Duque, Bladimiro Rincon-Orozco, Stelia C. Mendez-Sanchez
      First page: 24
      Abstract: Although there are existing vaccines against severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), new COVID-19 cases are increasing due to low immunization coverage and the emergence of new variants. For this reason, new drugs to treat and prevent severe COVID-19 are needed. Here, we provide four different FDA-approved drugs against SARS-CoV-2 proteins involved in the entry and replication process, aiming to identify potential drugs to treat COVID-19. We use the main protease (Mpro), the spike glycoprotein (S protein), and RNA-dependent RNA polymerase (RdRp) as protein targets for anti- SARS-CoV-2 drugs. In our constructed database, we selected different drugs against each target (Mpro, S protein, and RdRp) based on their common interactions with relevant residues involved in viral entry at the host cell and replication. Furthermore, their stability inside the binding pocket, as well as their predicted binding-free energy, allow us to provide new insight into the possible drug repurposing of viomycin (interacting with Mpro) due to its interactions with key residues, such as Asn 143, Glu 166, and Gln 189 at the same time as hesperidin (interacting with the S protein) is interacting with residues Tyr 449, Ser 494, and Thr 500, keeping inside the predicted binding pocket, as well as interacting with residues in different variants of concern. Finally, we also suggest nystatin and elvitegravir (interacting with RdRp) as possible drugs due to their stability within the predicted pocket along the simulation and their interaction with key residues, such as Asp 760, Asp 761, and Asp 618. Altogether our results provide new knowledge about the possible mechanism of the inhibition of viomycin, hesperidin, elvitegravir, and nystatin to inhibit the viral life cycle of SARS-CoV-2 and some of its variants of concern (VOC). Additionally, some iodide-based contrast agents were also found to bind the S protein strongly, i.e., iohexol (−58.99 Kcal/mol), iotrolan (−76.19 Kcal/mol), and ioxilan (−62.37 Kcal/mol). Despite the information we report here as the possible strong interaction between these contrast agents and the SARS-CoV-2′s S protein, Mpro, and RdRp, we believe that further investigation, including chemical modifications in their structures, are needed for COVID-19 treatment.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-04-14
      DOI: 10.3390/scipharm90020024
      Issue No: Vol. 90, No. 2 (2022)
  • Sci. Pharm., Vol. 90, Pages 25: Compounding in Ukraine: Assessment of the
           Risks for the Ointment’s Quality by the FMECA Method

    • Authors: Lesia Savchenko, Yuri Pidpruzhnykov, Roman Lesyk, Liudas Ivanauskas, Alla Kotvitska, Victoriya Georgiyants
      First page: 25
      Abstract: The level of compounded medicines (CM) quality has always been questioned in different countries. This problem has been resolved by the introduction of quality assurance system (QAS) standards. One of its main areas of significance is the risks assessment process, which is especially important for the compounding pharmacy according to the requirements of different international documents. Since ointments constitute a large part of CM, quantity assessment of risks for their quality by the FMECA method has been completed. During the first step of the research, 42 potential deviations of compounded ointments (CO) quality were identified. Via the questioning of compounding pharmacies specialists in different regions of Ukraine by a pre-developed ten-point scale, the severity of deviations consequence, their occurrence probability, and detecting possibility were determined followed by the calculation of the priority risk number (PRN) value. The Pareto analysis showed that nine possible CO quality defects represented 21% of their total number. Defects related to the composition or technology of ointments (29%) and their compliance with microbiological purity requirements (23%) had the largest percentage contribution to the total PRN value. It was also found that the deviations consequence had the most serious impact on the CO quality, due to their direct influence on patient health.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-04-19
      DOI: 10.3390/scipharm90020025
      Issue No: Vol. 90, No. 2 (2022)
  • Sci. Pharm., Vol. 90, Pages 26: Binding of GS-461203 and Its Halogen
           Derivatives to HCV Genotype 2a RNA Polymerase Drug Resistance Mutants

    • Authors: Muhammad Arba, Setyanto Tri Wahyudi, Muhammad Sulaiman Zubair, Dylan Brunt, Mursalin Singh, Chun Wu
      First page: 26
      Abstract: Hepatitis C Virus (HCV) is reported to develop GS-461203 resistance because of multiple mutations within the RNA-dependent RNA Polymerase (RdRp) of HCV. The lack of a high-resolution structure of these RdRp mutants in complex with GS-461203 hinders efforts to understand the drug resistance. Here we decipher the binding differences of GS-461203 in the wild type and mutated systems T179A or M289L of HCV RdRp Genotype 2a using homology modeling, molecular docking, and molecular dynamics simulation. Key residues responsible for GS-461203 binding were identified to be Arg48, Arg158, Asp318, Asp319, and Asp220, and that mutations T179A or M289L have caused conformational changes of GS-461203 in the RdRp active site. The affinities of GS-461203 were reduced in T179A system, but it became slightly stronger in the M289L system. Furthermore, we designed two new analogues of GS-461203 which encouragingly induced more stable interactions than GS-461203, and thus resulted in much better binding energies. This present study reveals how a single mutation, T179A or M289L, will modulate GS-461203 binding in HCV RdRp Genotype 2a, while introducing two novel analogues to overcome the drug resistance which may be good candidate for further experimental verification.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-04-21
      DOI: 10.3390/scipharm90020026
      Issue No: Vol. 90, No. 2 (2022)
  • Sci. Pharm., Vol. 90, Pages 27: Purification of Andrographolide Methanolic
           Extract Using Molecularly Imprinted Polymer Prepared by Precipitation

    • Authors: Wiwin Winingsih, Slamet Ibrahim, Sophi Damayanti
      First page: 27
      Abstract: Molecularly Imprinted Polymer (MIP) has a specific cavity in which the conformity of shape, size, and functionalities corresponds with its template molecule and has been widely used in separation processes. Therefore, this study aims to examine the application of MIP for the purification of andrographolide. The MIP was synthesized by precipitation polymerization using methacrylic acid (MAA) and ethylene glycol dimethacrylate (EGDMA) as the functional monomer and cross-linker, andrographolide as a template, and acetonitrile:toluene (3:1) as porogen solvent. The results showed that the binding capacity of Synthesized MIP was 1.2486 mg/g, while the particle size was 295.5 nm with a polydispersity index of 0.064. Furthermore, the imprinting and selectivity factors were 1.148 and 12.37, respectively. The purification process by MIP increased the purity from 55.37 ± 0.69 to 94.94% ± 0.34, while the isolate characterization showed that purified andrographolide had a similar character compared to the standard.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-04-26
      DOI: 10.3390/scipharm90020027
      Issue No: Vol. 90, No. 2 (2022)
  • Sci. Pharm., Vol. 90, Pages 28: Preclinical Safety Profile of an Oral
           Naringenin/Hesperidin Dosage Form by In Vivo Toxicological Tests

    • Authors: Carla Georgina Cicero-Sarmiento, Rolffy Ortiz-Andrade, Jesús Alfredo Araujo-León, Maira Rubí Segura-Campos, Priscila Vazquez-Garcia, Héctor Rubio-Zapata, Efrén Hernández-Baltazar, Victor Yañez-Pérez, Amanda Sánchez-Recillas, Juan Carlos Sánchez-Salgado, Emanuel Hernández-Núñez, Durcy Ruiz-Ciau
      First page: 28
      Abstract: We developed a naringenin–hesperidin molar mixture (MIX–160) with proven antihyperglycemic and vasorelaxant activity in preclinical studies. A solid dosage form was manufactured to improve the bioavailability properties. In the current study, we sought to evaluate the oral preclinical toxicity of the MIX–160 dosage form, which showed no mortality or significant changes in the body weight, food consumption and tissue/organ mass in rats. Three daily oral doses (50, 300 and 2000 mg/kg of MIX–160) were assayed for 28 days. The results showed no structural abnormalities in the histological analysis and no significant changes (p > 0.05) in the liver biochemical markers (total bilirubin, AST and ALT) compared to the control group. The above findings showed that the MIX–160 dosage form did not exhibit relevant toxic effects, which suggests its potential safety as a drug candidate for clinical studies.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-05-02
      DOI: 10.3390/scipharm90020028
      Issue No: Vol. 90, No. 2 (2022)
  • Sci. Pharm., Vol. 90, Pages 29: Gossypol from Gossypium spp. Inhibits
           Helicobacter pylori Clinical Strains and Urease Enzyme Activity:
           Bioactivity and Safety Assessments

    • Authors: Miroslava Šudomová, Sherif T. S. Hassan
      First page: 29
      Abstract: This study investigates the inhibitory activities of gossypol, a natural polyphenolic compound from Gossypium spp., against Helicobacter pylori (HP) clinical strains and a urease enzyme that plays a key role in the pathogenesis of HP. Gossypol was detected to exhibit a bacteriostatic action against all the HP strains tested with minimum inhibitory concentration (MIC) values ranging from 3.51 to 4.14 µg/mL. The activity of HP urease (HPU) was efficiently impeded by gossypol with a 50% inhibitory concentration (IC50) value of 3.3 µM using an Electrospray Ionization–Mass Spectrometry (ESI-MS)-based method. The in vitro cytotoxicity assay showed no significant cytotoxic properties of gossypol against human gastric epithelial cells. Additionally, molecular docking studies were performed to assess the binding mode and the molecular interactions of gossypol with HPU with a binding affinity value of −8.1 kcal/mol compared with an HPU–acetohydroxamic acid (a standard urease inhibitor) docking complex (–6.1 kcal/mol). The overall results reveal that gossypol might help fight against HP infection by two mechanisms of action: inhibition of the growth of HP and inhibition of urease.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-05-05
      DOI: 10.3390/scipharm90020029
      Issue No: Vol. 90, No. 2 (2022)
  • Sci. Pharm., Vol. 90, Pages 30: Cinnamomum bejolghota Extract Inhibits
           Colorectal Cancer Cell Metastasis and TGF-β1-Induced

    • Authors: Athicha Kittiwattanokhun, Sukanda Innajak, Etsu Tashiro, Masaya Imoto, Ramida Watanapokasin
      First page: 30
      Abstract: Cinnamomum bejolghota, used in Thai traditional medicine remedies, has several biological activities including antimicrobial, antifungal, and anticancer. In colorectal cancer, epithelial-mesenchymal transition (EMT) is an initial step of cancer metastasis. Thus, this study investigated the effects of C. bejolghota bark extract (CBE) on colorectal cancer cell metastasis and transforming growth factor-β1 (TGF-β1) induced EMT in LoVo cells. The results showed that CBE could reduce cell migration, invasion, and adhesion of LoVo cells in a dose-dependent manner. In addition, our studies also showed that CBE could reverse TGF-β1-induced morphological changes as well as increase an epithelial marker, E-cadherin, while the expression of the mesenchymal marker, N-cadherin, was decreased in TGF-β1-treated LoVo cells. MMP-2 expression was effectively decreased but TIMP-1 and TIMP-2 expression was increased by the CBE treatment in LoVo cells. CBE also inhibited Smad2/3 phosphorylation and nuclear translocation as well as decreased the expression of Snail, Slug, and TCF8/ZEB1 transcription factors in LoVo cells. Moreover, CBE could inhibit TGF-β1-induced Smad-independent signaling pathway by decreased phosphorylation of ERK1/2, p38, and Akt. These findings suggest that CBE inhibited TGF-β1-induced EMT in LoVo cells via both Smad-dependent and Smad-independent pathways. Therefore, CBE may function as an alternative therapeutic treatment for colorectal cancer metastasis.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-05-09
      DOI: 10.3390/scipharm90020030
      Issue No: Vol. 90, No. 2 (2022)
  • Sci. Pharm., Vol. 90, Pages 31: Antifungal and Modulatory Activity of
           Lemon Balm (Lippia alba (MILL.) N. E. BROWN) Essential Oil

    • Authors: Gleilton Sales, Suelen Medeiros, Igor Soares, Tiago Sampaio, Mary Bandeira, Nádia Nogueira, Maria Queiroz
      First page: 31
      Abstract: Fungal diseases and the progressive development of resistance are a challenge. In this context, Lippia alba (lemon balm) is a species used in folk medicine, being described with antimicrobial potential. The aim of this study was to determine the antifungal activity and modulating effect of the essential oil of Lippia alba (Mill.) N.E. Brown leaves (LaEO). The antifungal activity of LaEO on eight Candida strains was determined by minimum inhibitory concentration (MIC) and minimum lethal concentration (MLC), minimum biofilm inhibition concentration (MBIC), minimum biofilm eradication concentration (MBEC) and time-kill. The checkerboard technique was used to determine the modulating effect of LaEO on antifungal activity. The results indicate the presence of 11 constituents, with a predominance of carvone (58.15%) and limonene (25.37%). LaEO was able to inhibit the growth of all tested microorganisms, with MIC and MLC ranging from 0.078 to 1.25 mg/mL and MBIC and MBEC ranging from 0.156 to 5 mg/mL. The time-kill assay showed that LaEO was able to eliminate the strains after two hours of exposure and the best association was observed for the combination of LaEO and ketoconazole. The results of the study indicate that LaEO has excellent antifungal activity with potential biotechnological application.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-05-11
      DOI: 10.3390/scipharm90020031
      Issue No: Vol. 90, No. 2 (2022)
  • Sci. Pharm., Vol. 90, Pages 32: Comparison of the Purity and Impurity of
           Glucagon-for-Injection Products under Various Stability Conditions

    • Authors: Zhongli Bao, Ya-Chi Cheng, Mary Ziping Luo, Jack Yongfeng Zhang
      First page: 32
      Abstract: Glucagon is a polypeptide hormone that serves as an essential therapeutic agent in the emergency treatment of hypoglycemia. Recently, the first generic glucagon for injection was approved. However, unlike its brand name counterpart, which is produced via recombinant DNA, the generic glucagon is produced using a chemical synthesis method. Regardless of its origin, impurities may occur in both glucagon drug products. While these impurities may greatly compromise the safety and efficacy of the glucagon drug products, studies accessing the impurities of glucagon for injection are limited. This manuscript analyzed the stability and impurities of a generic and brand glucagon for injection, including desamido and non-desamido impurities, under various storage and temperature conditions using an ultra-performance liquid chromatography method. The glucagon products were analyzed after 6 and 24 months of storage under room temperatures (20–25 °C). In addition, the products were also assessed after 6 months of storage under high temperatures (40 °C). Under each stability storage condition, three lots of the synthetic glucagon were evaluated by UPLC with at least one lot of the recombinant glucagon for comparison. A total of 37 peaks were identified (except for the solvent peaks, which appeared at retention times less than 1.5 min) from the synthetic and recombinant glucagon lots. It was found that the number of impurities observed in the synthetic glucagon were lower than the referenced recombinant glucagon across all stability conditions. Throughout all tested conditions, the synthetic glucagon for injection had an averaged purity of 92.8–99.3%, while the referenced recombinant drug had an averaged purity of 70.3–91.7%. Based on the study results, it can be concluded that the impurity profile for the synthetic glucagon for injection has a comparable and even lower level of impurities than the recombinant version under all stability conditions.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-05-17
      DOI: 10.3390/scipharm90020032
      Issue No: Vol. 90, No. 2 (2022)
  • Sci. Pharm., Vol. 90, Pages 33: Quality and In Vivo Assessment of a Fulvic
           Acid Complex: A Validation Study

    • Authors: Rahmuddin Khan, Pooja Jain, Foziyah Zakir, Mohd Aqil, Sameer Alshehri, Mohd Aamir Mirza, Zeenat Iqbal
      First page: 33
      Abstract: The present work aimed to re-assess the bioavailability enhancement potential of fulvic acid (FA). Carbamazepine (CBZ) and peat were used as a model drug and FA source, respectively. Our group has already evaluated the bioavailability enhancement potential of a less commercially viable source of FA, i.e., shilajit. In the present work, the phase solubility of CBZ was analyzed with varying concentrations of peat-sourced FA (2–12% w/v). The prepared complex (CBZ-FA) was characterized by X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC). Dissolution, pharmacokinetic, and pharmacodynamic studies were also carried out. The results showed the presence of an interaction between the drug and FA within the complex, which led to 98.99 ± 2.0% enhancement in drug solubility. The results also showed 79.23 ± 2.1% dissolution of the complexed drug over 60 min and 69.32 ± 2.2% permeation from the intestinal gut sac over 90 min, which led to a significant enhancement of bioavailability and a reduction in the duration of epileptic seizures. Thus, this study re-authenticates our earlier results and suggests switching the FA source (shilajit to peat) for commercial product development.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-05-19
      DOI: 10.3390/scipharm90020033
      Issue No: Vol. 90, No. 2 (2022)
  • Sci. Pharm., Vol. 90, Pages 34: Quality by Design: A Suitable Methodology
           in Industrial Pharmacy for Costa Rican Universities

    • Authors: Luis Castillo-Henríquez, Brayan Murillo-Castillo, Lexi Chaves-Siles, Juan José Mora-Román, Nils Ramírez-Arguedas, Édgar Hernández-Mora, José Vega-Baudrit
      First page: 34
      Abstract: This review aims to present the Quality by Design (QbD) model as a suitable methodology to perform research in the academic Costa Rican institutions that teach Pharmacy. Pubmed, Science Direct, and Google Scholar databases were screened for original research papers and review papers published not more than ten years ago. Institutional repositories from the different universities were reviewed as well. The QbD model stands out as a great methodology for carrying out research projects regarding Pharmaceutical Sciences, but especially for Industrial Pharmacy, where it has contributed in terms of formulation development, manufacturing, and quality control. Academic research based on this model enables the training and development of practical, scientific, and leadership skills in Industrial Pharmacy students. The generated knowledge can be shared in classrooms, which represents an ideal environment to communicate research results and to foster collaborative work between researchers, professors, and students. Moreover, research performed through a QbD approach increases the confidence shown by the industrial sector and health regulatory authorities in the quality of the research, products, and knowledge that are developed and created in an Academy. As a result, the implementation of the model has allowed the creation, transfer, and materialization of knowledge from the Costa Rican Academy to different local pharmaceutical industries.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-05-19
      DOI: 10.3390/scipharm90020034
      Issue No: Vol. 90, No. 2 (2022)
  • Sci. Pharm., Vol. 90, Pages 35: Concepts for New Rapid Simple HPLC Method
           for Quantification of Fosfomycin Trometamol in Pharmaceutical Dosage Forms
           with Direct UV Detection

    • Authors: Marjan Piponski, Tanja Bakovska Stoimenova, Tetiana Melnyk, Sergiy Kovalenko, Elena Lazarevska Todevska, Marjan Velkovski, Sami El Deeb, Yuriy Mysula, Liliya Logoyda
      First page: 35
      Abstract: Two different concepts for developing direct HPLC-UV methods for quantifying fosfomycin trometamol were developed without any derivatization and modification of the analyte. In the first concept, without the use of alkylamines as ion-pairs in the mobile phase, by using cyanopropyl CN and a strong anion-exchanger column, we investigated the possibility of their highly polar and anion-exchanging forces and mechanisms to retain, separate and detect trometamol without the help of additional agents or modifiers. In the second concept, the most frequent reversed-phase C18 columns with different characteristics and vendors were tested in combination with different length-based alkylamines with 3–10 C atoms in their chains. In our research, we found that the ion-pairing of fosfomycin with 6–10 C-atom-based alkyl-length of aliphatic chains manifested the most appropriate strength of interactions between alkyl-paired trometamol molecules and octadecylsilane or C18 bonded RP column to achieve optimal retention, selectivity and peak shape on chromatograms, with the possibility for the fine-tuning of elution time. The simplicity of our method concept omits the need for expensive and sophisticated columns like HILIC, C30 graphite carbon, and mixed-mode-based columns for easier retaining, separation, and determination of fosfomycin, and for its quantification purposes, especially in high-throughput analyses in regular quality-control laboratories.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-05-24
      DOI: 10.3390/scipharm90020035
      Issue No: Vol. 90, No. 2 (2022)
  • Sci. Pharm., Vol. 90, Pages 36: Optimized Methods for Analytical and
           Functional Comparison of Biosimilar mAb Drugs: A Case Study for Avastin,
           Mvasi, and Zirabev

    • Authors: Büşra Gürel, Eda Çapkın, Ayhan Parlar, Aylin Özkan, Meltem Çorbacıoğlu, Duygu Emine Dağlikoca, Meral Yüce
      First page: 36
      Abstract: Bevacizumab is a humanized therapeutic monoclonal antibody used to reduce angiogenesis, a hallmark of cancer, by binding to VEGF-A. Many pharmaceutical companies have developed biosimilars of Bevacizumab in the last decade. The official reports provided by the FDA and EMA summarize the analytical performance of biosimilars as compared to the originators without giving detailed analytical procedures. In the current study, several key methods were optimized and reported for analytical and functional comparison of bevacizumab originators (Avastin, Altuzan) and approved commercial biosimilars (Zirabev and Mvasi). This case study presents a comparative analysis of a set of biosimilars under optimized analytical conditions for the first time in the literature. The chemical structure of all products was analyzed at intact protein and peptide levels by high-resolution mass spectrometry; the major glycoforms and posttranslational modifications, including oxidation, deamidation, N-terminal PyroGlu addition, and C-terminal Lys clipping, were compared. The SPR technique was used to reveal antigen and some receptor binding kinetics of all products, and the ELISA technique was used for C1q binding affinity analysis. Finally, the inhibition performance of the samples was evaluated by an MTS-based proliferation assay in vitro. Major glycoforms were similar, with minor differences among the samples. Posttranslational modifications, except C-terminal Lys, were determined similarly, while unclipped Lys percentage was higher in Zirabev. The binding kinetics for VEGF, FcRn, FcγRIa, and C1q were similar or in the value range of originators. The anti-proliferative effect of Zirabev was slightly higher than the originators and Mvasi. The analysis of biosimilars under the same conditions could provide a new aspect to the literature in terms of the applied analytical techniques. Further studies in this field would be helpful to better understand the inter-comparability of the biosimilars.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-05-31
      DOI: 10.3390/scipharm90020036
      Issue No: Vol. 90, No. 2 (2022)
  • Sci. Pharm., Vol. 90, Pages 37: Ex Vivo and In Vivo Study of Some
           Isoquinoline Precursors

    • Authors: Miglena Milusheva, Vera Gledacheva, Margarita Batmazyan, Stoyanka Nikolova, Iliyana Stefanova, Darinka Dimitrova, Kremena Saracheva, Desislav Tomov, Veneta Chaova-Gizdakova
      First page: 37
      Abstract: This article concerns the synthesis and biological activities of some N-(1-(3,4-dimethoxyphenyl)propan-2-yl) amides as isoquinoline precursors and compounds with smooth muscle (SM) relaxant activity. Aim: find the biological activity of N-(1-(3,4-dimethoxyphenyl)propan-2-yl) amides and compare it with papaverine, an isoquinoline alkaloid that has been known as a brain and coronary vasodilator and SM relaxant. Materials and methods: In silico simulation with the PASS online program predicts SM relaxant activity for the compounds. The amides were tested on the isolated gastric SM preparations (SMPs) from rats to determine their effects on spontaneous contractile activity (CA) compared with papaverine. The in vivo effect on the learning and memory processes of rats was also assessed. Results: the data from the isometric measurements showed that one of the compounds caused ex vivo relaxation in circular SM tissues isolated from the stomach (corpus) of male Wistar rats. Conclusion: We found that the compound’s SM relaxation uses the papaverine pathway. It also has an improving effect on the cognitive functions of learning and memory processes in rats.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-06-13
      DOI: 10.3390/scipharm90020037
      Issue No: Vol. 90, No. 2 (2022)
  • Sci. Pharm., Vol. 90, Pages 38: In Vitro and In Silico Antistaphylococcal
           Activity of Indole Alkaloids Isolated from Tabernaemontana cymosa Jacq

    • Authors: Yina Pájaro-González, Julián Cabrera-Barraza, Geraldine Martelo-Ramírez, Andrés F. Oliveros-Díaz, Juan Urrego-Álvarez, Wiston Quiñones-Fletcher, Fredyc Díaz-Castillo
      First page: 38
      Abstract: The species of the genus Tabernaemontana have a long tradition of use in different pathologies of infectious origins; the antibacterial, antifungal, and antiviral effects related to the control of the pathologies where the species of this genus are used, have been attributed to the indole monoterpene alkaloids, mainly those of the iboga type. There are more than 1000 alkaloids isolated from different species of Tabernaemontana and other genera of the Apocynaceae family, several of which lack studies related to antibacterial activity. In the present study, four monoterpene indole alkaloids were isolated from the seeds of the species Tabernaemontana cymosa Jacq, namely voacangine (1), voacangine-7-hydroxyindolenine (2), 3-oxovoacangine (3), and rupicoline (4), which were tested in an in vitro antibacterial activity study against the bacteria S. aureus, sensitive and resistant to methicillin, and classified by the World Health Organization as critical for the investigation of new antibiotics. Of the four alkaloids tested, only voacangine was active against S. aureus, with an MIC of 50 µg/mL. In addition, an in silico study was carried out between the four isolated alkaloids and some proteins of this bacterium, finding that voacangine also showed binding to proteins involved in cell wall synthesis, mainly PBP2 and PBP2a.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-06-14
      DOI: 10.3390/scipharm90020038
      Issue No: Vol. 90, No. 2 (2022)
  • Sci. Pharm., Vol. 90, Pages 5: A New Practice to Monitor the Fabrication
           Process of Fab-Targeting Ligands from Bevacizumab by LC-MS: Preparation
           and Analytical Characterization

    • Authors: Franck Marquet, Valentina D’Atri, Davy Guillarme, Gerrit Borchard
      First page: 5
      Abstract: The objective of this study was to qualitatively evaluate a Fab-targeting ligand preparation containing free thiol groups in the hinge region by using bevacizumab as a model. The evaluation focused on the purification of fragments through a nonaffinity-based process using a centrifugal ultrafiltration technique and mild reduction conditions for the intact production of F(ab’) fragments with specific inter-heavy-chain disulfide bonds cleavage. Under these conditions, F(ab’) fragments with a defined chemical composition were successfully obtained via proteolytic digestion followed by a controlled reduction reaction process maintaining the integrity of the binding sites. The ultrafiltration purification technique appears to be suitable for the removal of the digestive enzyme but inefficient for the removal of Fc fragments, thus requiring additional processing. A suitable analytical strategy was developed, allowing us to demonstrate the reformation of disulfide bridges between the two reduced cysteines within F(ab’) fragments.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-01-04
      DOI: 10.3390/scipharm90010005
      Issue No: Vol. 90, No. 1 (2022)
  • Sci. Pharm., Vol. 90, Pages 6: Dehydroepiandrosterone (DHEA) Improves the
           Metabolic and Haemostatic Disturbances in Rats with Male Hypogonadism

    • Authors: Sally M. Safwat, Abdelaziz M. Hussein, Elsayed A. Eid, Mohamed S. Serria, Basem H. Elesawy, Hussein F. Sakr
      First page: 6
      Abstract: Objectives: The current work was designed to study the effect of dehydroepiandrosterone (DHEA) on glucose homeostasis, liver functions and hemostatic disturbances in a rat model of bilateral orchidectomy (ORCH). Methods: 32 male rats (n = 8) were randomly assigned into 4 groups; (i) control (sham operated) group; were normal rats in which all surgical procedures were done without ORCH, (ii) Control + DHEA group: as control group but rats were treated with DHEA for 12 weeks, (iii) orchiectomized (ORCH) group: rats had bilateral orchidectomy and (iv) ORCH + DHEA group: orchiectomized rats treated with DHEA for 12 weeks. Four weeks after ORCH, DHEA treatment began and lasted for twelve weeks. By the end of the experiment, the parameters of glucose homeostasis, lipid profile, liver enzymes, bleeding and clotting times (B.T. and C.T.), prothrombin time (P.T.), activated partial thromboplastin time (aPTT), platelet count and aggregation, von-Willebrand factor (vWF), fibrinogen, plasminogen activator inhibitor (PAI-1), fibrin degradation products (FDP), intercellular adhesion molecule (ICAM-1), vascular cell adhesion molecule (VCAM-1), endothelin-1 were measured. Results: ORCH caused significant deteriorations in the parameters of glucose homeostasis, lipid profile, and liver functions (p < 0.05). In addition, lower androgenicity-induced by ORCH caused a significant rise in PAI-1, fibrinogen, FDPs, ET-1 (p < 0.01) with significant shortening of bleeding and clotting times. DHEA replacement therapy significantly decreased glucose, insulin, PAI-1, fibrinogen, ICAM-1, and VCAM-1 when compared to ORCH rats. Conclusion: DHEA ameliorated the metabolic, hepatic, hypercoagulable, and hypofibrinolysis disturbances induced by ORCH.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-01-20
      DOI: 10.3390/scipharm90010006
      Issue No: Vol. 90, No. 1 (2022)
  • Sci. Pharm., Vol. 90, Pages 7: Antineoplastic Activity of Water-Soluble
           Form of Novel Kinase Inhibitor
           immobilized on Polymeric Poly(PEGMA-co-DMM) Carrier

    • Authors: Nataliya Finiuk, Olga Klyuchivska, Nataliya Mitina, Halyna Kuznietsova, Kateryna Volianiuk, Alexander Zaichenko, Volodymyr Rybalchenko, Rostyslav Stoika
      First page: 7
      Abstract: The maleimide derivative 1-(4-chlorobenzyl)-3-chloro-4-(3-trifluoromethylphenylamino)-1H-pyrrole-2,5-dione (MI-1) was synthesized as inhibitor of several protein kinases, however, its application is hindered by its poor water solubility. In this study, the mechanisms of the antineoplastic action of MI-1 and its MI-1/M5 complex with M5 carrier (poly (PEGMA-co-DMM)) towards human colon carcinoma HCT116 cells were investigated by using the MTT and clonogenic assays, DNA intercalation with methyl green replacement, alkaline DNA comet assay, and Western-blot analysis. MI-1 compound and its MI-1/M5 complex possessed high toxicity towards colon (HCT116), cervical (HeLa) carcinoma cells and melanoma (SK-MEL-28) cells with GI50 value in a range of 0.75–7.22 µg/mL, and demonstrated high selectivity index (SI ˃ 6.9). The p53 status of colon cancer cells did not affect the sensitivity of these cells to the treatment with MI-1 and its MI-1/M5 complex. M5 polymer possessed low toxicity towards studied cells. The MI-1, MI-1/M5, and M5 only slightly inhibited growth of the pseudo-normal HaCaT and Balb/c 3T3 cell lines (GI50 ˃ 50 μg/mL). The MI-1 and its MI-1/M5 complex induced mitochondria-dependent pathway of apoptosis, damage of the DNA, and morphological changes in HCT116 cells, and affected the G2/M transition checkpoint. The MI-1 intercalated into the DNA molecule, while such capability of MI-1/M5 complex and M5 polymer was much lower. Thus, poly (PEGMA-co-DMM) might be a promising carrier for delivery of the maleimide derivative, MI-1, a novel kinase inhibitor, through improving its solubility in aqueous media and enhancing its antiproliferative action towards human tumor cells. Studies are in progress on the treatment of Nemeth-Kellner lymphoma (NK/Ly)-bearing mice with the MI-1 and MI-1/M5 complex.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-01-21
      DOI: 10.3390/scipharm90010007
      Issue No: Vol. 90, No. 1 (2022)
  • Sci. Pharm., Vol. 90, Pages 8: Pharmacokinetic Study of Mucoadhesive
           Itopride Hydrochloride In Situ Nasal Gel Formulations in a Comparative In
           Vivo Study and Histopathological Safety Evaluation

    • Authors: Maha A. Marzouk, Dina A. Osman, Amany I. Abd El-Fattah, Reem A. Aldeeb
      First page: 8
      Abstract: Hepatic first-pass metabolism has been a major cause of reduced bioavailability for many drugs. Using the nasal route as an alternative route to deliver drugs to the systemic circulation provided the solution to this problem. One of the drugs which are highly affected by first-pass metabolism is itopride hydrochloride (ITO HCl). It is a prokinetic agent used for the treatment of various gastrointestinal motility disorders, mainly gastroesophageal reflux. The objective of this study was to determine the pharmacokinetic parameters of selected mucoadhesive in situ nasal gel formulations (F1 and F17) of itopride hydrochloride (ITO HCl) and to evaluate their safety after topical application on the nasal mucosa. The tested formulations contained 18% w/v poloxamer 407 with 0.5% w/v of HPMC K4M (F1), or with 0.5% w/v MC (F17). A randomized cross-over study was done on six rabbits after administration of F1, F17, and commercial oral tablets (Ganaton®). Plasma levels were assessed using high-performance liquid chromatography (HPLC) to compare the nasal gel formulations with the conventional oral tablets. Histopathological study of the nasal mucosa was performed in rats after nasal application of both in situ gel formulas. The in vivo pharmacokinetic profiles of in situ nasal gel formulas F1 and F17 provided showed improvement in Cmax, Ke, t1/2, AUC0–24, AUC24–inf, AUC0–inf, AUMC24–inf, AUMC0–inf, MRT, Vd, and Cmax/AUC0–24 values over commercial tablets (p < 0.05). No statistically significant difference was found between both nasal gel formulas (F1 and F17). The percentage relative bioavailability of ITO HCl nasal in situ gel F1 and F17 was found to be 171.22% and 178.91%, respectively, in comparison with the commercial tablet. Histopathological study of the nasal mucosa revealed the safety of nasal in situ gel formulations to the nasal mucosa after 14 days of application. The study showed that the formulation of itopride hydrochloride as a mucoadhesive in situ nasal gel has enhanced the drug bioavailability due to avoidance of first-pass metabolism. The study points to the potential of mucoadhesive nasal in situ gel in terms of safety and efficiency.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-01-21
      DOI: 10.3390/scipharm90010008
      Issue No: Vol. 90, No. 1 (2022)
  • Sci. Pharm., Vol. 90, Pages 9: Acknowledgment to Reviewers of Scientia
           Pharmaceutica in 2021

    • Authors: Scientia Pharmaceutica Editorial Office Scientia Pharmaceutica Editorial Office
      First page: 9
      Abstract: Rigorous peer-reviews are the basis of high-quality academic publishing [...]
      Citation: Scientia Pharmaceutica
      PubDate: 2022-01-27
      DOI: 10.3390/scipharm90010009
      Issue No: Vol. 90, No. 1 (2022)
  • Sci. Pharm., Vol. 90, Pages 10: Antioxidant Activity, Sun Protection
           Activity, and Phytochemical Profile of Ethanolic Extracts of Daemonorops
           acehensis Resin and Its Phytosomes

    • Authors: Rita Kartika Sari, Yanico Hadi Prayogo, Salman Arib Rozan, Mohamad Rafi, Ietje Wientarsih
      First page: 10
      Abstract: Daemonorops (Indonesian: jernang) resin is one of Indonesia’s leading non-timber forest products and can be developed as a source of natural antioxidants and sun protection. This study aimed to select promising solvents for extracting a Daemonorops acehensis resin and phytosome formulation with high antioxidant capacities and sun protection factor (SPF) values. Jernang resin was extracted using a water–ethanol mixture in five different ratios. The promising extract was then mixed with soy lecithin in three different formulations. A promising extract and phytosome were then selected based on their antioxidant capacities and sun protection factor (SPF) values. A liquid chromatography mass spectrometry/mass spectrometry (LC–MS/MS) analysis was also performed on five extracts to identify the components in the extracts that might be responsible for the biological activity. The results showed that the ethanol solvent variation and phytosome formulation influenced the antioxidant capacity and SPF value. A hundred-percent ethanolic extract and F1 phytosome exhibited the highest antioxidant capacities and SPF values. A qualitative analysis revealed the various classes of compounds in the extract and phytosome. A flavylium chromophore, dracorhodin, dominated the resin extract and was presumed to be the marker compound responsible for their antioxidant capabilities and SPF values. These findings are important for manufacturing sunscreens containing active compounds of bioactive natural resins.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-02-03
      DOI: 10.3390/scipharm90010010
      Issue No: Vol. 90, No. 1 (2022)
  • Sci. Pharm., Vol. 90, Pages 11: Proof-of-Concept Preclinical Use of
           Drosophila melanogaster in the Initial Screening of Immunomodulators

    • Authors: Firzan Nainu, Muh. Akbar Bahar, Sartini Sartini, Reski Amalia Rosa, Nur Rahmah, Reski Amelia Kamri, Nur Rahma Rumata, Risfah Yulianty, Elly Wahyudin
      First page: 11
      Abstract: Drug discovery is a complex process, and the use of a comprehensive approach is deemed necessary to discover new chemical entities with novel mechanisms of action. This research was carried out to determine whether Drosophila melanogaster can serve as an appropriate model organism in the initial screening of drug candidates with immunomodulatory activities. To test this, we performed phenotypic assay and molecular analysis to investigate the immunomodulatory activities of aspirin, dexamethasone, curcumin, and epigallocatechin gallate (EGCG), that have been reported to yield such effects in the mammalian model system. In vivo survival analysis demonstrated that all drugs/compounds were relatively safe at the tested concentrations. In the infection assay, curcumin and EGCG showed a protective signature to bacterial infection in flies lacking Toll-mediated immune responses. Furthermore, dexamethasone and aspirin, drugs with immunosuppressive activity, could improve the survival of PGRP-LBΔ mutant flies with hyperactivated immune system. These phenotypes were supported by RT-qPCR-based molecular analysis, revealing that drugs/compounds used in this study could modulate the expression level of genes related to the immune system. In conclusion, while curcumin and EGCG could promote the improvement of fly survival against infection, aspirin and dexamethasone were able to suppress overactivation of immune responses in D. melanogaster. These results are in line with the ones observed in the mammalian model system, further emphasizing the notion that flies would serve as a prospective model organism in the initial screening of drug candidates for their immunomodulatory activities prior to further checking in the mammalian animal models. In the end, this will reduce the use of mammalian animal models for preliminary experiments in an effort to discover/repurpose drugs with immunomodulatory activity.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-02-08
      DOI: 10.3390/scipharm90010011
      Issue No: Vol. 90, No. 1 (2022)
  • Sci. Pharm., Vol. 90, Pages 12: Repurposing of Anti-Malarial Drug
           Quinacrine for Cancer Treatment: A Review

    • Authors: Makhan Kumar, Angshuman Sarkar
      First page: 12
      Abstract: Quinacrine (QC), a synthetic drug belonging to the 9-aminoacridine family, has been used extensively to treat malaria and multiple ailments over the past several decades. Following its discovery in the 1920s and extensive use for the treatment of malaria for nearly two decades, numerous studies have explored its antineoplastic potential in both preclinical and clinical settings. Multiple studies spanning over seven decades have examined a wide range of QC anticancer activities across various types of cancers, along with the underlying mechanisms. Many of these mechanisms, including activation of the p53 signaling cascade and simultaneous NF-κB signaling inhibition, have been reported in various studies, bringing QC to a unique polypharmacological category drug possessing the potential to treat a wide variety of diseases, including cancer. This article summarizes most of the research conducted over several decades to uncover new molecular mechanisms activated or inactivated and directly correlate with antineoplastic activity QC.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-02-08
      DOI: 10.3390/scipharm90010012
      Issue No: Vol. 90, No. 1 (2022)
  • Sci. Pharm., Vol. 90, Pages 13: Amphiphilic Alkylated Pectin Hydrogels for
           Enhanced Topical Delivery of Fusidic Acid: Formulation and In Vitro

    • Authors: Mohammad F. Bostanudin
      First page: 13
      Abstract: Hydrogels constructed of amphiphilically modified polysaccharides have attracted a lot of interest because of their potential to augment drug diffusion over the skin. This research describes the synthesis of amphiphilic alkylated pectin via glycidyl tert-butyl ether modification (alkylation degree 15.7%), which was characterized using spectroscopic and thermal analysis techniques and then formulated into hydrogels for the study of their potential in regulating fusidic acid diffusion topically. The hydrogels were formulated by the ionic interaction of negatively charged pectin and positively charged crosslinker CaCl2, with a reported fusidic acid loading degree of 93–95%. Hydrogels made of alkylated pectin showed a lower swelling percentage than that of native pectin, resulting in a slower fusidic acid release. The influence of pH on the swelling percentage and drug release was also investigated, with results revealing that greater pH enhanced swelling percentage and drug release. The in vitro interactions with HaCaT cells revealed negligible cytotoxicity under application-relevant settings. Utilizing Franz diffusion cells, the alkylated pectin hydrogels caused fusidic acid to penetrate the Strat-M® membrane at a 1.5-fold higher rate than the native pectin hydrogels. Overall, the in vitro results showed that alkylated pectin hydrogels have a lot of promise for topical distribution, which needs further investigation.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-02-14
      DOI: 10.3390/scipharm90010013
      Issue No: Vol. 90, No. 1 (2022)
  • Sci. Pharm., Vol. 90, Pages 14: Systematic Review on the Effectiveness of
           Essential and Carrier Oils as Skin Penetration Enhancers in Pharmaceutical

    • Authors: Bahjat Alhasso, Muhammad Usman Ghori, Barbara R. Conway
      First page: 14
      Abstract: Oils, including essential oils and their constituents, are widely reported to have penetration enhancement activity and have been incorporated into a wide range of pharmaceutical formulations. This study sought to determine if there is an evidence base for the selection of appropriate oils for particular applications and compare their effectiveness across different formulation types. A systematic review of the data sources, consisting of Google Scholar, EMBASE, PubMed, Medline, and Scopus, was carried out and, following screening and quality assessment, 112 articles were included within the analysis. The research was classified according to the active pharmaceutical ingredient, dosage form, in vitro/in vivo study, carrier material(s), penetration enhancers as essential oils, and other chemical enhancers. The review identified four groups of oils used in the formulation of skin preparations; in order of popularity, these are terpene-type essential oils (63%), fatty acid-containing essential oils (29%) and, finally, 8% of essential oils comprising Vitamin E derivatives and miscellaneous essential oils. It was concluded that terpene essential oils may have benefits over the fatty acid-containing oils, and their incorporation into advanced pharmaceutical formulations such as nanoemulsions, microemulsions, vesicular systems, and transdermal patches makes them an attractive proposition to enhance drug permeation through the skin.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-02-19
      DOI: 10.3390/scipharm90010014
      Issue No: Vol. 90, No. 1 (2022)
  • Sci. Pharm., Vol. 90, Pages 15: Formulation Optimization of Extemporaneous
           Oral Liquids Containing Naloxone and Propranolol for Pediatric Use

    • Authors: Maria Attebäck, Bengt Hedin, Sofia Mattsson
      First page: 15
      Abstract: There is a need to develop dosage forms suitable for children to improve drug treatment. Extemporaneous compounding of drugs for children is one way to meet these needs. However, excipients generally considered as safe in adults may not be appropriate in dosage forms intended for children. The aim was to optimize the composition of two pediatric liquid preparations by substituting paraben as a microbiological preservative and ethanol as a solubilizer, with excipients more suitable for pediatric use. The oral liquids were Naloxone 1 mg/mL and Propranolol 10 mg/mL. Twelve different formulations were tested with propranolol and naloxone, respectively, during the screening process to select appropriate formulations. Sodium benzoate and glycerol were used as a preservative and solubilizer, respectively, and different pH of the formulations were evaluated. The formulations were characterized according to dispensed dose (dosing accuracy), viscosity and osmolality. The optimized formulations from the screening process were tested with two amounts of sodium benzoate and microbiological assays were performed. These formulations were shown to have satisfactory preservative properties and dosing accuracy. The results showed that the oral liquids could be prepared without the addition of solubilizer and with lower osmolality (naloxone), thus reducing the risk of gastrointestinal side effects.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-02-22
      DOI: 10.3390/scipharm90010015
      Issue No: Vol. 90, No. 1 (2022)
  • Sci. Pharm., Vol. 90, Pages 16: Compatibility of Different Formulations in
           TrichoConceptTM Vehicles for Hair Treatments

    • Authors: Hudson Polonini, Sarah Taylor, Clark Zander
      First page: 16
      Abstract: The wide variety of potential pathogeneses for alopecia and the wide variety of active pharmaceutical ingredients (APIs) to treat and manage those pathogeneses highlight the importance of the development of stable and effective topical treatments. Topical options for alopecia on the market remain limited and oral products may result in unwanted systemic adverse effects. This study is meant to fill the gap by determining compatibility in terms of beyond-use date (BUD) of APIs with theoretical or demonstrated benefits for topical use for alopecia. The compatibility of seven formulations was tested: F1 = clobetasol 0.05% in TrichoWashTM; F2 = ketoconazole 2% in TrichoWashTM; F3 = spironolactone 1% in TrichoWashTM; F4 = latanoprost 0.1% in TrichoCreamTM; F5 = pyridoxine HCl 0.5%, vitamin A acetate 1%, and vitamin E succinate 12.1 IU in TrichoCondTM; F6 = Caffeine 2%, menthol 1%, and pyridoxine HCl 0.5% in TrichoWashTM; F7 = Latanoprost 0.1%, minoxidil 5%, and finasteride 0.25% in TrichoSolTM. All formulations presented a BUD of 6 months, except for F4 and F7, which showed compatibility for 3 months. This validates the compatibility of the APIs with the TrichotechTM vehicles, and that they are highly convenient for compounding pharmacies.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-02-25
      DOI: 10.3390/scipharm90010016
      Issue No: Vol. 90, No. 1 (2022)
  • Sci. Pharm., Vol. 90, Pages 17: Evaluation of Liposome-Loaded Microbubbles
           as a Theranostic Tool in a Murine Collagen-Induced Arthritis Model

    • Authors: Joke Deprez, Silke Roovers, Guillaume Lajoinie, Heleen Dewitte, Tine Decruy, Julie Coudenys, Benedicte Descamps, Christian Vanhove, Michel Versluis, Dirk Elewaut, Peggy Jacques, Stefaan C. De Smedt, Ine Lentacker
      First page: 17
      Abstract: Rheumatoid arthritis (RA) is an autoimmune disease characterized by severe inflammation of the synovial tissue. Here, we assess the feasibility of liposome-loaded microbubbles as theranostic agents in a murine arthritis model. First, contrast-enhanced ultrasound (CEUS) was used to quantify neovascularization in this model since CEUS is well-established for RA diagnosis in humans. Next, the potential of liposome-loaded microbubbles and ultrasound (US) to selectively enhance liposome delivery to the synovium was evaluated with in vivo fluorescence imaging. This procedure is made very challenging by the presence of hard joints and by the limited lifetime of the microbubbles. The inflamed knee joints were exposed to therapeutic US after intravenous injection of liposome-loaded microbubbles. Loaded microbubbles were found to be quickly captured by the liver. This resulted in fast clearance of attached liposomes while free and long-circulating liposomes were able to accumulate over time in the inflamed joints. Our observations show that murine arthritis models are not well-suited for evaluating the potential of microbubble-mediated drug delivery in joints given: (i) restricted microbubble passage in murine synovial vasculature and (ii) limited control over the exact ultrasound conditions in situ given the much shorter length scale of the murine joints as compared to the therapeutic wavelength.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-02-28
      DOI: 10.3390/scipharm90010017
      Issue No: Vol. 90, No. 1 (2022)
  • Sci. Pharm., Vol. 90, Pages 18: Purple Corn Silk Extract Attenuates
           UVB-Induced Inflammation in Human Keratinocyte Cells

    • Authors: Watcharaporn Poorahong, Sukanda Innajak, Malyn Ungsurungsie, Ramida Watanapokasin
      First page: 18
      Abstract: UVB is a causative factor for severe skin damage, such as cell aging, death, and inflammation. UVB easily permeates into the epidermis layer of human skin, which is mainly composed of keratinocyte cells. In previous results, we found that purple corn silk (PCS) extract showed the potential to inhibit keratinocyte damages of UVB-treated cells. Thus, in this study, we aimed to evaluate the preventive effects of PCS extract against the inflammation of UVB-induced keratinocyte cells using the HaCaT cell line. HaCaT cells were treated with PCS extract at various concentrations for 1 h, then exposed to 25 mJ/cm2 UVB before subsequent experiments. Fragmented DNA was observed using flow cytometry. The inflammatory response was investigated through NF-κB activity by immunofluorescence staining and related protein expression by Western blotting. The results demonstrated that PCS extract decreased the sub-G1 DNA content. Interestingly, PCS extract attenuated NF-κB activity via suppressed NF-κB nuclear translocation and protein expression. Moreover, PCS extract remarkably decreased c-Jun phosphorylation and decreased proinflammatory cytokines, along with iNOS and COX-2 levels in UVB-treated cells compared to the UVB-control group. This finding exhibited that PCS extract minimized inflammation in keratinocyte cells induced by UVB radiation.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-03-01
      DOI: 10.3390/scipharm90010018
      Issue No: Vol. 90, No. 1 (2022)
  • Sci. Pharm., Vol. 90, Pages 19: Application of Quality by Design Approach
           to the Pharmaceutical Development of Anticancer Crude Extracts of Crocus
           sativus Perianth

    • Authors: Olha Mykhailenko, Liudas Ivanauskas, Ivan Bezruk, Vilma Petrikaitė, Victoriya Georgiyants
      First page: 19
      Abstract: The application of the Quality by Design (QbD) concept to extracts obtained from Crocus sativus perianth with potential anticancer activity will ensure the safety, efficiency, and quality control of the entire technological process, as well as determine the critical factors affecting the quality of extracts. Potentially critical points of the production of the plant extracts, including the cultivation and processing of the plant materials, the extraction process, and the choice of solvents, were identified using the Ishikawa diagram and FMEA risk assessment methods as well as the corrective actions proposed. The Herbal Chemical Marker Ranking System (HerbMars) approach was used to justify the Q-markers choice of Crocus, which takes into account bioavailability, pharmacological activity, and the presence of the selected standard. An experimental design (DoE) was used to assess the influence of potentially critical factors on the efficiency of the compound extraction from raw materials with water or ethanol. The presence of 16 compounds in Crocus perianth was determined by HPLC and their quantitative assessment was established. Selected compounds (ferulic acid, mangiferin, crocin, rutin, isoquercitrin) can be used for the quality control of Crocus perianth. In addition, the stigmas from the Volyn region met the requirements of ISO 3632 for saffron as a spice (category I). The cytotoxic activity against melanoma (IGR39) and triple-negative breast cancer (MDA-MB-231) cell lines of the hydroethanolic extract of C. sativus perianth was significantly more pronounced than the water extract, probably due to the chemical composition of the constituent components. The results show that the QbD approach is a powerful tool for process development for the production of quality herbal drugs.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-03-03
      DOI: 10.3390/scipharm90010019
      Issue No: Vol. 90, No. 1 (2022)
  • Sci. Pharm., Vol. 90, Pages 20: Nanocarrier Systems in Taste Masking

    • Authors: Nasr Eldin Hussein Nasr, Aliaa Nabil ElMeshad, Ahmed Roshdy Fares
      First page: 20
      Abstract: Taste is the most crucial organoleptic parameter affecting patient compliance in the case of drugs with poor palatability. Taste masking is a major challenge for the development of orally ingested active pharmaceutical constituents in the pharmaceutical industry. Numerous conventional taste-masking techniques have been extensively studied. In parallel, affecting the drug solubility or release is a major concern of conventional taste-masking techniques. Recently, many nanocarrier systems have been introduced, claiming the advantage of effective taste masking without affecting either the drug solubility or its release. In this review, we will present new techniques for taste masking, including taste-masking techniques utilizing nanocarrier systems such as liposomes, polymeric and solid lipid nanoparticles, polymeric micelles, submicron lipid emulsions, and nanogels. We will chiefly highlight the composition of these systems and their applications in designing oral therapeutic delivery systems successful in masking the taste of bitter molecules.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-03-04
      DOI: 10.3390/scipharm90010020
      Issue No: Vol. 90, No. 1 (2022)
  • Sci. Pharm., Vol. 90, Pages 21: Temperature and pH-Dependent Behaviors of
           mAb Drugs: A Case Study for Trastuzumab

    • Authors: Fatma Sert, Defne Hız, Mert Gülmez, Selen Ezgi Cankurtaran, Cemre Irmak Kayalan, Hasan Kurt, Meral Yüce
      First page: 21
      Abstract: The distortions in the high-order structure of therapeutic monoclonal antibodies (mAbs) under different environmental conditions acutely affect mAb stability, resulting in altered safety, efficacy, and shelf-life profiles. The overall stability of mAbs depends on many factors, and it requires complementary techniques for an in-depth analysis. The stability of mAbs can be characterized by differential centrifugal sedimentation (DCS), differential scanning calorimetry (DSC), differential scanning fluorimetry (DSF), and size exclusion chromatography (SEC) techniques. In this report, temperature-ramped dynamic light scattering (DLS), and circular dichroism (CD) spectroscopy were employed as complementary tools to show how temperature and pH affect the aggregation of a model mAb, trastuzumab, in solution. The results showed that the aggregation onset temperature of trastuzumab defined by DLS was 75 °C, which decreases the amount of β-sheets and causes a slight increase in helix structures. Moreover, the melting temperature of trastuzumab was determined to be between 80–83 °C by temperature-ramped CD spectrophotometry, which is in line with the Tm of trastuzumab’s Fab region tested with DSC. Thus, unfolding and aggregation of trastuzumab start simultaneously at 75 °C, and unfolding triggers the aggregation. The temperature-ramped CD and DLS methods are robust tools to determine the thermal behavior of biosimilars in various solution conditions. Their complementary usage provides solid scientific background for regulatory applications and a better understanding of mAb instability and its relationship with structural changes.
      Citation: Scientia Pharmaceutica
      PubDate: 2022-03-21
      DOI: 10.3390/scipharm90010021
      Issue No: Vol. 90, No. 1 (2022)
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