Publisher: Hindawi   (Total: 343 journals)

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Showing 1 - 200 of 343 Journals sorted alphabetically
Abstract and Applied Analysis     Open Access   (Followers: 3, SJR: 0.343, CiteScore: 1)
Active and Passive Electronic Components     Open Access   (Followers: 8, SJR: 0.136, CiteScore: 0)
Advances in Acoustics and Vibration     Open Access   (Followers: 51, SJR: 0.147, CiteScore: 0)
Advances in Aerospace Engineering     Open Access   (Followers: 62)
Advances in Agriculture     Open Access   (Followers: 12)
Advances in Artificial Intelligence     Open Access   (Followers: 21)
Advances in Astronomy     Open Access   (Followers: 47, SJR: 0.257, CiteScore: 1)
Advances in Bioinformatics     Open Access   (Followers: 20, SJR: 0.565, CiteScore: 2)
Advances in Biology     Open Access   (Followers: 12)
Advances in Chemistry     Open Access   (Followers: 34)
Advances in Civil Engineering     Open Access   (Followers: 51, SJR: 0.539, CiteScore: 1)
Advances in Computer Engineering     Open Access   (Followers: 8)
Advances in Condensed Matter Physics     Open Access   (Followers: 11, SJR: 0.315, CiteScore: 1)
Advances in Decision Sciences     Open Access   (Followers: 4, SJR: 0.303, CiteScore: 1)
Advances in Electrical Engineering     Open Access   (Followers: 52)
Advances in Electronics     Open Access   (Followers: 101)
Advances in Emergency Medicine     Open Access   (Followers: 15)
Advances in Endocrinology     Open Access   (Followers: 6)
Advances in Environmental Chemistry     Open Access   (Followers: 10)
Advances in Epidemiology     Open Access   (Followers: 9)
Advances in Fuzzy Systems     Open Access   (Followers: 5, SJR: 0.161, CiteScore: 1)
Advances in Geology     Open Access   (Followers: 19)
Advances in Geriatrics     Open Access   (Followers: 6)
Advances in Hematology     Open Access   (Followers: 13, SJR: 0.661, CiteScore: 2)
Advances in Hepatology     Open Access   (Followers: 3)
Advances in High Energy Physics     Open Access   (Followers: 25, SJR: 0.866, CiteScore: 2)
Advances in Human-Computer Interaction     Open Access   (Followers: 21, SJR: 0.186, CiteScore: 1)
Advances in Materials Science and Engineering     Open Access   (Followers: 30, SJR: 0.315, CiteScore: 1)
Advances in Mathematical Physics     Open Access   (Followers: 8, SJR: 0.218, CiteScore: 1)
Advances in Medicine     Open Access   (Followers: 3)
Advances in Meteorology     Open Access   (Followers: 24, SJR: 0.48, CiteScore: 1)
Advances in Multimedia     Open Access   (Followers: 1, SJR: 0.173, CiteScore: 1)
Advances in Nonlinear Optics     Open Access   (Followers: 6)
Advances in Numerical Analysis     Open Access   (Followers: 9)
Advances in Nursing     Open Access   (Followers: 37)
Advances in Operations Research     Open Access   (Followers: 13, SJR: 0.205, CiteScore: 1)
Advances in Optical Technologies     Open Access   (Followers: 4, SJR: 0.214, CiteScore: 1)
Advances in Optics     Open Access   (Followers: 7)
Advances in OptoElectronics     Open Access   (Followers: 6, SJR: 0.141, CiteScore: 0)
Advances in Orthopedics     Open Access   (Followers: 11, SJR: 0.922, CiteScore: 2)
Advances in Pharmacological and Pharmaceutical Sciences     Open Access   (Followers: 8, SJR: 0.591, CiteScore: 2)
Advances in Physical Chemistry     Open Access   (Followers: 13, SJR: 0.179, CiteScore: 1)
Advances in Polymer Technology     Open Access   (Followers: 14, SJR: 0.299, CiteScore: 1)
Advances in Power Electronics     Open Access   (Followers: 42, SJR: 0.184, CiteScore: 0)
Advances in Preventive Medicine     Open Access   (Followers: 6)
Advances in Public Health     Open Access   (Followers: 27)
Advances in Regenerative Medicine     Open Access   (Followers: 4)
Advances in Software Engineering     Open Access   (Followers: 11)
Advances in Statistics     Open Access   (Followers: 9)
Advances in Toxicology     Open Access   (Followers: 4)
Advances in Tribology     Open Access   (Followers: 15, SJR: 0.265, CiteScore: 1)
Advances in Urology     Open Access   (Followers: 13, SJR: 0.51, CiteScore: 1)
Advances in Virology     Open Access   (Followers: 8, SJR: 0.838, CiteScore: 2)
AIDS Research and Treatment     Open Access   (Followers: 2, SJR: 0.758, CiteScore: 2)
Analytical Cellular Pathology     Open Access   (Followers: 3, SJR: 0.886, CiteScore: 2)
Anatomy Research Intl.     Open Access   (Followers: 4)
Anemia     Open Access   (Followers: 6, SJR: 0.669, CiteScore: 2)
Anesthesiology Research and Practice     Open Access   (Followers: 15, SJR: 0.501, CiteScore: 1)
Applied and Environmental Soil Science     Open Access   (Followers: 18, SJR: 0.451, CiteScore: 1)
Applied Bionics and Biomechanics     Open Access   (Followers: 7, SJR: 0.288, CiteScore: 1)
Applied Computational Intelligence and Soft Computing     Open Access   (Followers: 14)
Archaea     Open Access   (Followers: 4, SJR: 0.852, CiteScore: 2)
Autism Research and Treatment     Open Access   (Followers: 34)
Autoimmune Diseases     Open Access   (Followers: 3, SJR: 0.805, CiteScore: 2)
Behavioural Neurology     Open Access   (Followers: 9, SJR: 0.786, CiteScore: 2)
Biochemistry Research Intl.     Open Access   (Followers: 6, SJR: 0.437, CiteScore: 2)
Bioinorganic Chemistry and Applications     Open Access   (Followers: 11, SJR: 0.419, CiteScore: 2)
BioMed Research Intl.     Open Access   (Followers: 5, SJR: 0.935, CiteScore: 3)
Biotechnology Research Intl.     Open Access   (Followers: 1)
Bone Marrow Research     Open Access   (Followers: 2, SJR: 0.531, CiteScore: 1)
Canadian J. of Gastroenterology & Hepatology     Open Access   (Followers: 4, SJR: 0.867, CiteScore: 1)
Canadian J. of Infectious Diseases and Medical Microbiology     Open Access   (Followers: 8, SJR: 0.548, CiteScore: 1)
Canadian Respiratory J.     Open Access   (Followers: 3, SJR: 0.474, CiteScore: 1)
Cardiology Research and Practice     Open Access   (Followers: 11, SJR: 1.237, CiteScore: 4)
Cardiovascular Therapeutics     Open Access   (Followers: 2, SJR: 1.075, CiteScore: 2)
Case Reports in Anesthesiology     Open Access   (Followers: 11)
Case Reports in Cardiology     Open Access   (Followers: 8, SJR: 0.219, CiteScore: 0)
Case Reports in Critical Care     Open Access   (Followers: 12)
Case Reports in Dentistry     Open Access   (Followers: 7, SJR: 0.229, CiteScore: 0)
Case Reports in Dermatological Medicine     Open Access   (Followers: 2)
Case Reports in Emergency Medicine     Open Access   (Followers: 17)
Case Reports in Endocrinology     Open Access   (Followers: 2, SJR: 0.209, CiteScore: 1)
Case Reports in Gastrointestinal Medicine     Open Access   (Followers: 3)
Case Reports in Genetics     Open Access   (Followers: 2)
Case Reports in Hematology     Open Access   (Followers: 9)
Case Reports in Hepatology     Open Access   (Followers: 2)
Case Reports in Immunology     Open Access   (Followers: 6)
Case Reports in Infectious Diseases     Open Access   (Followers: 6)
Case Reports in Medicine     Open Access   (Followers: 3)
Case Reports in Nephrology     Open Access   (Followers: 5)
Case Reports in Neurological Medicine     Open Access   (Followers: 1)
Case Reports in Obstetrics and Gynecology     Open Access   (Followers: 11)
Case Reports in Oncological Medicine     Open Access   (Followers: 2, SJR: 0.204, CiteScore: 1)
Case Reports in Ophthalmological Medicine     Open Access   (Followers: 3)
Case Reports in Orthopedics     Open Access   (Followers: 6)
Case Reports in Otolaryngology     Open Access   (Followers: 7)
Case Reports in Pathology     Open Access   (Followers: 7)
Case Reports in Pediatrics     Open Access   (Followers: 7)
Case Reports in Psychiatry     Open Access   (Followers: 17)
Case Reports in Pulmonology     Open Access   (Followers: 3)
Case Reports in Radiology     Open Access   (Followers: 12)
Case Reports in Rheumatology     Open Access   (Followers: 10)
Case Reports in Surgery     Open Access   (Followers: 12)
Case Reports in Transplantation     Open Access  
Case Reports in Urology     Open Access   (Followers: 12)
Case Reports in Vascular Medicine     Open Access  
Case Reports in Veterinary Medicine     Open Access   (Followers: 5)
Child Development Research     Open Access   (Followers: 20, SJR: 0.144, CiteScore: 0)
Chinese J. of Engineering     Open Access   (Followers: 2, SJR: 0.114, CiteScore: 0)
Chinese J. of Mathematics     Open Access  
Chromatography Research Intl.     Open Access   (Followers: 5)
Complexity     Hybrid Journal   (Followers: 7, SJR: 0.531, CiteScore: 2)
Computational and Mathematical Methods in Medicine     Open Access   (Followers: 2, SJR: 0.403, CiteScore: 1)
Computational Biology J.     Open Access   (Followers: 7)
Computational Intelligence and Neuroscience     Open Access   (Followers: 13, SJR: 0.326, CiteScore: 1)
Concepts in Magnetic Resonance Part A     Open Access   (Followers: 1, SJR: 0.354, CiteScore: 1)
Concepts in Magnetic Resonance Part B, Magnetic Resonance Engineering     Open Access   (Followers: 1, SJR: 0.26, CiteScore: 1)
Conference Papers in Science     Open Access   (Followers: 2)
Contrast Media & Molecular Imaging     Open Access   (Followers: 2, SJR: 0.842, CiteScore: 3)
Critical Care Research and Practice     Open Access   (Followers: 13, SJR: 0.499, CiteScore: 1)
Current Gerontology and Geriatrics Research     Open Access   (Followers: 9, SJR: 0.512, CiteScore: 2)
Depression Research and Treatment     Open Access   (Followers: 19, SJR: 0.816, CiteScore: 2)
Dermatology Research and Practice     Open Access   (Followers: 4, SJR: 0.806, CiteScore: 2)
Diagnostic and Therapeutic Endoscopy     Open Access   (SJR: 0.201, CiteScore: 1)
Discrete Dynamics in Nature and Society     Open Access   (Followers: 6, SJR: 0.279, CiteScore: 1)
Disease Markers     Open Access   (Followers: 1, SJR: 0.9, CiteScore: 2)
Economics Research Intl.     Open Access   (Followers: 1)
Education Research Intl.     Open Access   (Followers: 19)
Emergency Medicine Intl.     Open Access   (Followers: 10, SJR: 0.298, CiteScore: 1)
Enzyme Research     Open Access   (Followers: 5, SJR: 0.653, CiteScore: 3)
Evidence-based Complementary and Alternative Medicine     Open Access   (Followers: 29, SJR: 0.683, CiteScore: 2)
Game Theory     Open Access   (Followers: 1)
Gastroenterology Research and Practice     Open Access   (Followers: 1, SJR: 0.768, CiteScore: 2)
Genetics Research Intl.     Open Access   (Followers: 1, SJR: 0.61, CiteScore: 2)
Geofluids     Open Access   (Followers: 5, SJR: 0.952, CiteScore: 2)
Hepatitis Research and Treatment     Open Access   (Followers: 6, SJR: 0.389, CiteScore: 2)
Heteroatom Chemistry     Open Access   (Followers: 3, SJR: 0.333, CiteScore: 1)
HPB Surgery     Open Access   (Followers: 7, SJR: 0.824, CiteScore: 2)
Infectious Diseases in Obstetrics and Gynecology     Open Access   (Followers: 5, SJR: 1.27, CiteScore: 2)
Interdisciplinary Perspectives on Infectious Diseases     Open Access   (Followers: 1, SJR: 0.627, CiteScore: 2)
Intl. J. of Aerospace Engineering     Open Access   (Followers: 78, SJR: 0.232, CiteScore: 1)
Intl. J. of Agronomy     Open Access   (Followers: 6, SJR: 0.311, CiteScore: 1)
Intl. J. of Alzheimer's Disease     Open Access   (Followers: 12, SJR: 0.787, CiteScore: 3)
Intl. J. of Analytical Chemistry     Open Access   (Followers: 22, SJR: 0.285, CiteScore: 1)
Intl. J. of Antennas and Propagation     Open Access   (Followers: 11, SJR: 0.233, CiteScore: 1)
Intl. J. of Atmospheric Sciences     Open Access   (Followers: 21)
Intl. J. of Biodiversity     Open Access   (Followers: 3)
Intl. J. of Biomaterials     Open Access   (Followers: 5, SJR: 0.511, CiteScore: 2)
Intl. J. of Biomedical Imaging     Open Access   (Followers: 3, SJR: 0.501, CiteScore: 2)
Intl. J. of Breast Cancer     Open Access   (Followers: 14, SJR: 1.025, CiteScore: 2)
Intl. J. of Cell Biology     Open Access   (Followers: 4, SJR: 1.887, CiteScore: 4)
Intl. J. of Chemical Engineering     Open Access   (Followers: 8, SJR: 0.327, CiteScore: 1)
Intl. J. of Chronic Diseases     Open Access   (Followers: 1)
Intl. J. of Combinatorics     Open Access   (Followers: 1)
Intl. J. of Computer Games Technology     Open Access   (Followers: 10, SJR: 0.287, CiteScore: 2)
Intl. J. of Corrosion     Open Access   (Followers: 11, SJR: 0.194, CiteScore: 1)
Intl. J. of Dentistry     Open Access   (Followers: 8, SJR: 0.649, CiteScore: 2)
Intl. J. of Differential Equations     Open Access   (Followers: 8, SJR: 0.191, CiteScore: 0)
Intl. J. of Digital Multimedia Broadcasting     Open Access   (Followers: 5, SJR: 0.296, CiteScore: 2)
Intl. J. of Electrochemistry     Open Access   (Followers: 10)
Intl. J. of Endocrinology     Open Access   (Followers: 4, SJR: 1.012, CiteScore: 3)
Intl. J. of Engineering Mathematics     Open Access   (Followers: 7)
Intl. J. of Food Science     Open Access   (Followers: 5, SJR: 0.44, CiteScore: 2)
Intl. J. of Forestry Research     Open Access   (Followers: 3, SJR: 0.373, CiteScore: 1)
Intl. J. of Genomics     Open Access   (Followers: 2, SJR: 0.868, CiteScore: 3)
Intl. J. of Geophysics     Open Access   (Followers: 5, SJR: 0.182, CiteScore: 1)
Intl. J. of Hepatology     Open Access   (Followers: 4, SJR: 0.874, CiteScore: 2)
Intl. J. of Hypertension     Open Access   (Followers: 8, SJR: 0.578, CiteScore: 1)
Intl. J. of Inflammation     Open Access   (SJR: 1.264, CiteScore: 3)
Intl. J. of Inorganic Chemistry     Open Access   (Followers: 4)
Intl. J. of Manufacturing Engineering     Open Access   (Followers: 2)
Intl. J. of Mathematics and Mathematical Sciences     Open Access   (Followers: 3, SJR: 0.177, CiteScore: 0)
Intl. J. of Medicinal Chemistry     Open Access   (Followers: 6, SJR: 0.31, CiteScore: 1)
Intl. J. of Metals     Open Access   (Followers: 7)
Intl. J. of Microbiology     Open Access   (Followers: 8, SJR: 0.662, CiteScore: 2)
Intl. J. of Microwave Science and Technology     Open Access   (Followers: 3, SJR: 0.136, CiteScore: 1)
Intl. J. of Navigation and Observation     Open Access   (Followers: 20, SJR: 0.267, CiteScore: 2)
Intl. J. of Nephrology     Open Access   (Followers: 2, SJR: 0.697, CiteScore: 1)
Intl. J. of Oceanography     Open Access   (Followers: 8)
Intl. J. of Optics     Open Access   (Followers: 9, SJR: 0.231, CiteScore: 1)
Intl. J. of Otolaryngology     Open Access   (Followers: 3)
Intl. J. of Partial Differential Equations     Open Access   (Followers: 2)
Intl. J. of Pediatrics     Open Access   (Followers: 6)
Intl. J. of Peptides     Open Access   (Followers: 2, SJR: 0.46, CiteScore: 1)
Intl. J. of Photoenergy     Open Access   (Followers: 3, SJR: 0.341, CiteScore: 1)
Intl. J. of Plant Genomics     Open Access   (Followers: 4, SJR: 0.583, CiteScore: 1)
Intl. J. of Polymer Science     Open Access   (Followers: 28, SJR: 0.298, CiteScore: 1)
Intl. J. of Population Research     Open Access   (Followers: 4)
Intl. J. of Quality, Statistics, and Reliability     Open Access   (Followers: 17)
Intl. J. of Reconfigurable Computing     Open Access   (SJR: 0.123, CiteScore: 1)
Intl. J. of Reproductive Medicine     Open Access   (Followers: 6)
Intl. J. of Rheumatology     Open Access   (Followers: 4, SJR: 0.645, CiteScore: 2)
Intl. J. of Rotating Machinery     Open Access   (Followers: 2, SJR: 0.193, CiteScore: 1)
Intl. J. of Spectroscopy     Open Access   (Followers: 8)
Intl. J. of Stochastic Analysis     Open Access   (Followers: 3, SJR: 0.279, CiteScore: 1)
Intl. J. of Surgical Oncology     Open Access   (Followers: 1, SJR: 0.573, CiteScore: 2)
Intl. J. of Telemedicine and Applications     Open Access   (Followers: 6, SJR: 0.403, CiteScore: 2)
Intl. J. of Vascular Medicine     Open Access   (SJR: 0.782, CiteScore: 2)
Intl. J. of Zoology     Open Access   (Followers: 2, SJR: 0.209, CiteScore: 1)
Intl. Scholarly Research Notices     Open Access   (Followers: 235)

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Similar Journals
Journal Cover
Advances in Pharmacological and Pharmaceutical Sciences
Journal Prestige (SJR): 0.591
Citation Impact (citeScore): 2
Number of Followers: 8  

  This is an Open Access Journal Open Access journal
ISSN (Print) 2633-4682 - ISSN (Online) 2633-4690
Published by Hindawi Homepage  [343 journals]
  • Computational Evaluation of the Inhibition Efficacies of HIV Antivirals on
           SARS-CoV-2 (COVID-19) Protease and Identification of 3D Pharmacophore and
           Hit Compounds

    • Abstract: Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the novel coronavirus behind the fast-spreading coronavirus disease 2019 (COVID-19). Pharmaceutical researchers are currently researching medications or preventive vaccines that may be used to treat and combat the spread of COVID-19. Health practitioners all over the world are treating patients with currently available antiviral drugs, primarily the protease inhibitors used for HIV treatment. The present study mainly aims to evaluate the potencies of eight anti-HIV drugs to inhibit coronavirus protease using in silico methods. Derivation of pharmacophore, identification of hit molecules, and checking their virtual inhibition efficacies on the COVID-19 protease were also carried out in the present investigation. Classification of eight drug molecules (atazanavir, darunavir, fosamprenavir (amprenavir—metabolised product), saquinavir, lopinavir, ritonavir, nelfinavir, and indinavir) based on their molecular structures was completed and reported. The X-ray crystallographic structure of the main protease of coronavirus (SARS-CoV-2 protease) was obtained from the Protein Data Bank and prepared for computational studies using Edu PyMOL software. Docking studies were performed with AutoDock Vina software, and the results were evaluated with Discovery Studio software. The binding scores of the drugs on protease followed the order saquinavir > nelfinavir > lopinavir = indinavir > darunavir > amprenavir > ritonavir > atazanavir. Web servers such as PharmaGist and ZINCPharmer were employed to derive the 3D pharmacophore and to identify potential hit compounds, respectively. The identified hit molecules were docked with the SARS-CoV-2 protease and analysed. A detailed account of the type of interaction between the protease and the molecules is discussed. The majority of hit compounds displayed appreciable binding affinities on coronavirus protease. Three hit compounds possess structures similar to that of natural products, viz., flavonoids, and nucleoside. These molecules were hydrophilic and slightly deviated from Lipinski parameters. All other derived molecules obeyed the Lipinski rule. In vitro, in vivo, and toxicological studies of these compounds have to be performed before checking the actual druggability of these compounds.
      PubDate: Mon, 21 Sep 2020 15:05:02 +000
       
  • Antihypernociceptive, Anxiolytic, and Antidepressant Properties of Aqueous
           and Ethanol Extracts of Dissotis thollonii Cogn. (Melastomataceae) in Mice
           

    • Abstract: Diabetic neuropathy, which affects 7 to 9% of the world’s population and that is usually accompanied by anxiety and depression, is chronic pain that results from impaired function of the central or peripheral nervous system. This study aimed at evaluating the antihypernociceptive, antiallodynic, anxiolytic, and antidepressant effects of Dissotis thollonii extracts. Diabetic neuropathy was induced by intraperitoneal injection of streptozotocin (200 mg/kg) in mice. The aqueous and ethanol extracts (250 and 500 mg/kg) were administered orally. Hyperalgesia (thermal and chemical), allodynia (mechanical and thermal), anxiety (high plus labyrinth, light-dark box, and social interaction), and depression (open field test, suspension test tail, and forced swimming test) were evaluated, and then the levels of some cytokines and growth factors were determined. The aqueous and ethanol extracts of Dissotis thollonii demonstrated significant antihypernociceptive (inhibition of hyperalgesia and allodynia), anxiolytic, and antidepressant activities in mice made diabetic by STZ. The extracts also significantly inhibited () the levels of TNF-α, IL-1β, and IL-6 in the blood as well as the levels of TNF-α, IL-1β, IL-6, IGF, and NGF in the sciatic nerve. This study shows that the extracts of Dissotis thollonii have antihypernociceptive and neuroprotective effects which could be linked to the inhibition of proinflammatory cytokines and growth factors in the blood and the sciatic nerve.
      PubDate: Mon, 21 Sep 2020 15:05:02 +000
       
  • Hair Washing Formulations from Aloe elegans Todaro Gel: The Potential for
           Making Hair Shampoo

    • Abstract: This study aimed to describe the gross phytochemical constituents of Aloe elegans Todaro gel and evaluate the characteristics and quality of lab-made hair washing formulations prepared from the gel to show its potential in formulating hair washing shampoos. A. elegans gel mass was prepared from mature, healthy leaves collected from natural stand. Samples of 100% methanol extract of the gel were subjected to standard phytochemical screening and gas chromatography-mass spectroscopy (GC-MS) analysis. Five hair washing formulations (Fs) were, likewise, prepared by mixing 4.0–10.0 mL of gel with one (0.05 mL) to two (0.10 mL) drops of six synthetic and natural ingredients, namely, coconut oil, jojoba oil, olive oil, pure glycerin oil, lemon juice, and vitamin E. The gel to the total ingredient ratios (v/v) of the five formulations were 93 : 7 (F1), 94.5 : 5.5 (F2), 96.4 : 3.6 (F3), and 96.6 : 3.4 (F4 and F5). The formulations were evaluated using sensory inspection and common physicochemical methods. The phytochemical screening and GC-MS analysis revealed that A. elegans gel is the source of important chemical constituents used in the formulation of shampoos and similar products including saponins, capric acid, lauric acid, myristic acid, palmitic acid, linoleic acid, stearic acid, and phytol. Lab-made A. elegans hair washing formulations, especially those with 96.4–96.6% gel, were found to have similar characteristics and qualities with a common marketed shampoo. All the formulations were turbid with characteristic odor as the marketed shampoo. The pH values of the hair washing formulations (6.4–4.6) were comparable to those of the marketed shampoo (6.7). Formulations with higher proportion of gel had better foam stability, higher solid content (26–29%), higher surface tension (33–38 dynes/cm), shorter wetting time (150–160 sec), equivalent viscosities (26.45–26.73 poise), and conditioning performance than the marketed shampoo. These findings demonstrate that A. elegans gel mass can be used in the formulation of good-quality hair washing shampoos. We recommend future studies that aim to develop the phytochemical profile of the plant and a refined protocol of hair washing shampoo formulation.
      PubDate: Tue, 01 Sep 2020 01:50:07 +000
       
  • Comparative Study of Leaf and Rootstock Aqueous Extracts of Foeniculum
           vulgare on Chemical Profile and In Vitro Antioxidant and Antihyperglycemic
           Activities

    • Abstract: Foeniculum vulgare is a medicinal plant used in Moroccan folk medicine to treat several diseases such as diabetes. The aim of this study was to determine the phenolic bioactive compounds and to evaluate the antioxidant and antihyperglycemic activities of Foeniculum vulgare leaf and rootstock extracts. Phenolic compounds of F. vulgare rootstock and leaf extracts were determined using HPLC-DAD-QTOFMS analysis. The antioxidant activity was evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2’-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS•+) radicals. Moreover, the in vitro antihyperglycemic effects were tested by measuring the inhibition of α-amylase and α-glucosidase activities. HPLC-DAD-QTOFMS analysis identified thirty-two phenolic components in both leaf and rootstock extracts. Caffeic acid, quinic acid, and chlorogenic acid were the major compounds of F. vulgare leaf extract (FVLE), while the main compound of F. vulgare rootstock extracts (FVRE) was quinic acid. In the DPPH assay, F. vulgare leaf extract showed important antioxidant activity (IC50 = 12.16 ± 0.02 μg/mL) than F. vulgare rootstock extract (IC50 = 34.36 ± 0.09 μg/mL). Moreover, fennel leaf extracts revealed also the most powerful antioxidant activity (IC50 = 22.95 ± 0.4 μg/mL) in the ABTS assay. The in vitro antihyperglycemic activity showed that F. vulgare rootstock extract exhibited a remarkable inhibitory capacity (IC50 = 194.30 ± 4.8 μg/mL) of α-amylase compared with F. vulgare leaf extract (IC50 = 1026.50 ± 6.5 μg/mL). Furthermore, the inhibition of α-glucosidase was more importantly with F. vulgare rootstock (IC50 of 165.90 ± 1.2 μg/mL) than F. vulgare leaf extracts (203.80 ± 1.3 μg/mL). The funding of this study showed that F. vulgare rootstock and leaf extracts presented several phenolic compounds and showed important antioxidant and antidiabetic effects. We suggest that the identified molecules are responsible for the obtained activities. However, further studies focusing on the isolation and the determination of antioxidant and antidiabetic effects of F. vulgare rootstock and leaf main compounds are required.
      PubDate: Tue, 01 Sep 2020 01:35:07 +000
       
  • Activities of Some Medicinal Plants on the Proliferation and Invasion of
           Brain Tumor Cell Lines

    • Abstract: Cancer is a debilitating disease that is on the increase in both developed and developing countries. Anticancer drugs are often expensive, have narrow spectrum of activities, and are associated with toxicities and side effects such as myelosuppression, immunosuppression, gastrointestinal disturbance, alopecia, skin toxicity, and hepatotoxicity. Plants have been the major source of anticancer drugs both in orthodox and traditional medicine. Many of the plants claimed by the traditional medicine practitioners (TMPs) to be effective in the treatment of cancer are yet to be evaluated scientifically. In this work, five medicinal plants used by TMPs in Borno State, Nigeria, were tested against two brain tumor cell lines. Ethanol extracts of Securidaca longepedunculata, Andira inermis subsp. rooseveltii, Annona senegalensis, Carissa edulis, and Parinari polyandra were used. U87 and U231 brain tumor cell lines were used for proliferation assay, U251 cell line was used for the invasion assay in collagen V coated inserts, and U87 cell line was used for the western blot detection of cleaved Poly-ADP-Ribose-Polymerase (PARP). The result revealed that all tested extracts significantly () inhibited the proliferation of U87 and U231 cell lines with the respective IC50 values ranging between 8 and 20 μg/ml for S. longepedunculata and 100 and 90 μg/ml for P. polyandra. The five extracts significantly () inhibited the invasion of U251 cell line at the concentration of 10 μg/ml (S. longepedunculata), 20 μg/ml (A. inermis), 50 μg/ml (A. senegalensis), 50 μg/ml (C. edulis), and 50 μg/ml (P. polyandra). Securidaca longepedunculata extract induced the cleavage of PARP. It was concluded that these medicinal plants have antiproliferative and anti-invasive activities and possess good prospects as source of anticancer agents especially S. longepedunculata which induced apoptosis in U87 cell line.
      PubDate: Thu, 27 Aug 2020 09:35:08 +000
       
  • Current Status of Alginate in Drug Delivery

    • Abstract: Alginate is one of the natural polymers that are often used in drug- and protein-delivery systems. The use of alginate can provide several advantages including ease of preparation, biocompatibility, biodegradability, and nontoxicity. It can be applied to various routes of drug administration including targeted or localized drug-delivery systems. The development of alginates as a selected polymer in various delivery systems can be adjusted depending on the challenges that must be overcome by drug or proteins or the system itself. The increased effectiveness and safety of sodium alginate in the drug- or protein-delivery system are evidenced by changing the physicochemical characteristics of the drug or proteins. In this review, various routes of alginate-based drug or protein delivery, the effectivity of alginate in the stem cells, and cell encapsulation have been discussed. The recent advances in the in vivo alginate-based drug-delivery systems as well as their toxicities have also been reviewed.
      PubDate: Thu, 06 Aug 2020 15:35:01 +000
       
  • Ameliorative Effect of Vernonia amygdalina Plant Extract on Heavy
           Metal-Induced Liver and Kidney Dysfunction in Rats

    • Abstract: Heavy metal toxicity contributes to liver and kidney dysfunction and damage through oxidative stress mechanisms; however, from previous studies, extracts from the Vernonia amygdalina plant have shown to possess potent antioxidant properties. This study was aimed at uncovering the potential ameliorative effects of ethanolic extract from Vernonia amygdalina plant in heavy metal toxicity-induced liver and kidney dysfunction. For this study, 44 Sprague Dawley rats were divided into three groups. The control group received a basal diet and water only while the treatment groups received varied dosages of the heavy metals. The copper (Cu) and lead (Pb) groups had five subgroups. The Cu only and Cu recovery subgroups were administered with 16 mg/kg Cu intraperitoneally daily for 14 days, whereas the Pb only and Pb recovery subgroups were administered with 13 mg/kg Pb intraperitoneally daily for 14 days. Subsequently, the Pb only and Cu only subgroups were sacrificed. The three Pb and Cu treatment subgroups received oral graded doses (100 mg/kg, 200 mg/kg, and 300 mg/kg) of the extract for 21 days. The Cu recovery and Pb recovery subgroups were left to recover for 21 days. After histological examinations, the Pb and Cu pretreatment groups showed evidence of focal necrosis accompanied by inflammatory cell infiltrations. The serum levels of liver biomarkers AST, ALT, and GGT, as well as urea and creatinine, were significantly elevated () following copper and lead exposure. Upon posttreatment of the rats with the extract, the physiological levels of the biomarkers were restored and tissue architecture of the organs improved. Thus, the ethanolic extract of Vernonia amygdalina is capable of ameliorating the effects of heavy metal toxicity through potent antioxidative mechanisms.
      PubDate: Wed, 24 Jun 2020 07:50:01 +000
       
  • Examination of WHO/INRUD Core Drug Use Indicators at Public Primary
           Healthcare Centers in Kisii County, Kenya

    • Abstract: Background. Irrational drug use is a global problem. However, the extent of the problem is higher in low-income countries. This study sets out to assess and characterize drug use at the public primary healthcare centers (PPHCCs) in a rural county in Kenya, using the World Health Organization/International Network for the Rational Use of Drugs (WHO/INRUD) core drug use indicators methodology. Methods. Ten PPHCCs were randomly selected. From each PPHCC, ninety prescriptions from October to December 2018 were sampled and data extracted. Three hundred (30 per PPHCC) patients and ten (1 per PPHCC) dispensers were also observed and interviewed. The WHO/INRUD core drug use indicators were used to assess the patterns of drug use. Results. The average number of drugs per prescription was 2.9 (SD 0.5) (recommended: 1.6–1.8), and the percentage of drugs prescribed by generic names was 27.7% (recommended: 100%); the percentage of prescriptions with an antibiotic was 84.8% (recommended: 20.0–26.8%), and with an injection prescribed was 24.9% (recommended: 13.4–24.1%). The percentage of prescribed drugs from the Kenya Essential Medicines List was 96.7% (recommended: 100%). The average consultation time was 4.1 min (SD 1.7) (recommended: ≥10 min), the average dispensing time was 131.5 sec (SD 41.5) (recommended: ≥90 sec), the percentage of drugs actually dispensed was 76.3% (recommended: 100%), the percentage of drugs adequately labeled was 22.6% (recommended: 100%), and the percentage of patients with correct knowledge of dispensed drugs was 54.7% (recommended: 100%). Only 20% of the PPHCCs had a copy of KEML available, and 80% of the selected essential drugs assessed were available. Conclusion. The survey shows irrational drug use practices, particularly polypharmacy, nongeneric prescribing, overuse of antibiotics, short consultation time, and inadequacy of drug labeling. Effective programs and activities promoting the rational use of drugs are the key interventions suggested at all the health facilities.
      PubDate: Fri, 19 Jun 2020 15:05:01 +000
       
  • Phytochemical Analysis, Antioxidant Activity, Antimicrobial Activity, and
           Cytotoxicity of Chaptalia nutans Leaves

    • Abstract: Context. Chaptalia nutans (L.) Pol. (family: Asteraceae) is widely used in traditional medicine as laxative and anticough medications and especially in the traumatisms, wounds, and hemorrhages in topical preparations. Objective. This work was to evaluate the chemical constitution of the hydromethanolic (30/70 methanol-water) macerating extract obtained from the leaves of C. nutans, as well as to study the antioxidant, antimicrobial, cytotoxic, and genotoxic activity of the species. Materials and methods. Phytochemical screening, antioxidant activity (total phenolic, total flavonoid, condensed tannins content, DPPH radical, and FRAP), antibacterial activity (P. aeruginosa, B. cereus, E. epidermidis, E. coli, S. aureus, E. faecalis, P. mirabilis, Candida glabrata (clinical isolate), Candida tropicalis (clinical isolate), C. krusei (clinical isolate), and C. albicans (clinical isolate)), and oxidative stress parameters (TBARS, carbonyl protein, and DCFH) were analyzed according to the literature. Toxicity of C. nutans was evaluated using an alternative method, D. melanogaster, as well as a locomotor assay. Results. The phytochemical screening test of methanolic leaves extract revealed the presence of alkaloids, coumarins, quaternary bases, phenolics, flavonoids, tannins, and free steroids. A quantitative phytochemical study indicated the total phenol (30.17 ± 1.44 mg/g), flavonoid (21.64 ± 0.66 mg/g), and condensed tannins (9.58 ± 0.99 mg/g). DPPH (345.41 ± 5.35 μg/mL) and FRAP (379.98 ± 39.25 μM FeSO4/mg sample) show to extract of C. nutans leaves an intermediate value, indicating moderate antioxidant activity of the extract. Antibacterial results revealed only a positive result (antimicrobial activity) for the hexane fraction which significantly inhibited the microorganisms E. epidermidis, C. tropicalis, C. glabrata, and C. krusei at a concentration of 1000 μg/mL. TBARS, carbonyl protein, and DCFH demonstrate that the extract has the ability to protect the cell from protein and lipid damage, as well as the inhibition of oxygen-derived radicals at the three concentrations tested: 0.1, 1, and 10 mg/mL. Regarding the toxicity of C. nutans extract against D. melanogaster, it was found that until the concentration of 15 mg/mL, the extract showed no toxicity and that the LC50 obtained was 24 mg/mL. Results show that the C. nutans extract leaves used to prevent PQ damage were effective in reducing flies’ mortality and improving locomotor capacity. Conclusion. Our studies demonstrated for the first time that C. nutans crude leaf extract has high antioxidant capacity both in vitro and in vivo through different analysis techniques. These results make it possible to infer future applications in the pharmacological area, evidenced by the low toxicity observed in D. melanogatser, as well as the ability to neutralize different sources of RONS.
      PubDate: Fri, 01 May 2020 02:20:04 +000
       
  • Attenuation of Age-Related Hepatic Steatosis by Dunaliella salina
           Microalgae in Senescence Rats through the Regulation of Redox Status,
           Inflammatory Indices, and Apoptotic Biomarkers

    • Abstract: Background. Hepatic steatosis is the most common type of chronic liver disease and is considered an established risk factor of major chronic diseases. Purpose. The present study aimed to investigate the effect of Dunaliella salina, a microalga and its isolated zeaxanthin on age-related hepatic steatosis as well as their underling mechanism. Study Design. Age-related hepatic steatosis was induced in rats by intraperitoneal injection of D-galactose (200 mg/kg/day) for eight consecutive weeks. D. salina biomass (BDS; 450 mg/kg), its polar fraction (PDS; 30 mg/kg), carotenoid fraction (CDS; 30 mg/kg), and isolated zeaxanthin heneicosylate (ZH; 250 μg/kg) were orally administered to D-galactose treated rats for two weeks. Methods. Blood samples were collected 24 hours after the last dose of D. salina treatments, animals were sacrificed, and liver tissues were isolated. Sera as well as hepatic tissue homogenates were used for further investigations. Liver tissues were also used for histopathological and immunohistochemical examinations. A computed virtual docking study for the biologically active candidates was performed to confirm the proposed mechanism of action. Results. Oral treatment of D-galactose-injected rats with BDS, PDS, CDS, or ZH ameliorated the serum hepatic function parameters as well as serum levels of adiponectin, apolipoprotein B 100, and insulin. Furthermore, D. salina decreased the hepatic lipid contents, redox status biomarkers, inflammatory cytokine, and showing antiapoptotic properties. Molecular docking of β-carotene and zeaxanthin on various receptors involved in the pathophysiological cascade of steatosis highlighted the possible mechanism underlying the observed therapeutic effect. Conclusion. D. salina carotenoids have beneficial effect on age-related hepatic steatosis in senescence rats through the regulation of redox status, inflammatory indices, and apoptotic biomarkers.
      PubDate: Fri, 01 May 2020 01:50:03 +000
       
  • Antioxidant Action and In Vivo Anti-Inflammatory and Antinociceptive
           Activities of Myrciaria floribunda Fruit Peels: Possible Involvement of
           Opioidergic System

    • Abstract: This work evaluated the antioxidant properties and in vivo antinociceptive and anti-inflammatory effects of extracts obtained from fruit peels of Myrciaria floribunda (H. West ex Willd.) O. Berg (Myrtaceae). This plant is popularly known in Brazil as Cambuí or camboim. Different extracts were submitted to comparative analysis to determine the content of selected phytochemical classes (levels of total phenols, flavonoids, and monomeric anthocyanins) and the in vitro antioxidant potentials. The extract with higher potential was selected for in vivo evaluation of its antinociceptive and anti-inflammatory action. Finally, the chemical characterization of this extract was performed by high-performance liquid chromatography (HPLC). MfAE (extract obtained using acetone as solvent) showed the higher levels of phenols (296 mg GAE/g) and anthocyanins contents (35.65 mg Cy-3-glcE/g) that were associated with higher antioxidant activity. MfAE also exhibited in vivo anti-inflammatory and analgesic propertiers. This fraction inhibited the inflammatory and neurogenic phases of pain, and this effect was reversed by naloxone (suggesting the involvement of opioidergic system). MfAE reduced the abdominal contortions induced by acetic acid. The HPLC analysis revealed the presence of gallic acid (and its derivatives) and ellagic acid. Taken together, these data support the use of M. floribunda fruit peels for development of functional foods and nutraceutics.
      PubDate: Mon, 27 Apr 2020 13:20:03 +000
       
  • HPTLC Fingerprint Profile and Identification of Antidiabetic and
           Antioxidant Leads from Bauhinia rufescens L

    • Abstract: Diabetes is one of the world’s major health problems, and many reports have supported the role of oxidative stress in the pathogenesis of both type 1 and type 2 diabetes. The present study aims to evaluate the antidiabetic and antioxidant activity of Bauhinia rufescens, a plant used in Sudanese folkloric medicine for the treatment of diabetes. It was also aimed to identify isolates and characterize the bioactive antidiabetic and antioxidant compounds using bioactivity-guided fractionation followed by high-performance thin-layer chromatography (HPTLC) autobiography, liquid chromatography-mass spectrometric analysis, and nuclear magnetic resonance (NMR). Two potential compounds were successfully isolated and identified which may provide new leads for more potent analogues in drug discovery.
      PubDate: Fri, 24 Apr 2020 13:50:04 +000
       
  • Novel Dimethylacetamide-Containing Formulation Improves Infraorbital
           Anaesthesia Efficacy in Rats with Periodontitis

    • Abstract: Background. To evaluate acute toxicity and local anaesthetic activity of a formulation containing a novel dimethylacetamide derivative, antioxidant, and vasoconstrictor in rats with chronic periodontitis. Methods. Novel anaesthetic dimethylacetamide-containing formulation LHT-15-32 was studied as 2% water solution. Its acute intravenous and subcutaneous toxicity was determined in mice. Pain sensitivity threshold of the upper second molar was determined in rats with experimental periodontitis. Oxidative stress activity and total antioxidant capacity were determined in rats’ gingival mucosa by induced chemiluminescence. Local changes were evaluated in periodontal tissue by morphological examination. Tissue IL-1β, IL-10, and TNF-α concentration was quantitatively assessed by an enzyme-linked immunosorbent assay. LHT-15-31 Na-blocking activity was studied on isolated neurons of Limnaea stagnalis’ parapharyngeal ganglion. Isolated sciatic nerve of Rana radibunda was perfused with different concentrations of LHT-15-32 to assess its conductivity. Statistical analysis was used, and continuous variables were presented as mean ± square deviation. The normality of distribution was determined using ANOVA. Newman–Keuls parametric criterion was used for intergroup comparison. LD50 indexes were calculated by probit analysis. Results. LHT-15-32 acute intravenous and subcutaneous toxicity was lower than that of its active substance. The formulation by infraorbital administration induced deep dental anaesthesia which lasted over 70 min and activated the local antioxidant defense system and decreased IL-1β level in gingival tissue. LHT-15-32 triggered tissue reparation around the impacted upper molar in rats assessed five days after administration. At 10−6 to 10−3 M concentration, LHT-15-32 inhibited sciatic nerve conductivity and blocked Na+ channels of isolated neurons in a dose-dependent manner. Conclusions. The formulation may be considered as an effective and safe approach to anaesthetize upper molars with periodontitis.
      PubDate: Tue, 14 Apr 2020 07:20:00 +000
       
  • The Class III PI3K/Beclin-1 Autophagic Pathway Participates in the
           mmLDL-Induced Upregulation of ETA Receptor in Mouse Mesenteric Arteries

    • Abstract: Minimally modified low-density lipoprotein (mmLDL) is a risk factor for cardiovascular diseases. The current study explored the effect of mmLDL on the endothelin type A (ETA) receptor in mouse mesenteric arteries in vivo, as well as the role of autophagy in this process. mmLDL was injected via the caudal vein, and the Class III PI3K autophagic pathway inhibitor 3-methyladenine (3-MA) was injected intraperitoneally. The animals were divided into physiological saline (NS), mmLDL, and mmLDL + 3-MA groups. The dose-effect curve of endothelin-1- (ET-1-) induced mesenteric artery contraction was measured using myography, while ETA receptor mRNA expression was detected using real-time polymerase chain reactions, and the protein levels of the ETA receptor, class III PI3K, Beclin-1, LC3 II/I, p62, NF-κB, and p-NF-κB were observed using Western blot analysis. mmLDL significantly strengthened ET-1-induced contraction (the Emax value increased from 184.87 ± 7.46% in the NS group to 319.91 ± 20.31% in the mmLDL group (), and the pEC50 value increased from 8.05 ± 0.05 to 9.11 ± 0.09 (). In addition to upregulating the protein levels of Class III PI3K, Beclin-1, and LC3 II/I and downregulating that of p62, mmLDL significantly increased the mRNA expression and protein level of the ETA receptor and increased the protein level of p-NF-κB. However, these effects were significantly inhibited by 3-MA. mmLDL activates autophagy via the Class III PI3K/Beclin-1 pathway and upregulates the ETA receptor via the downstream NF-κB pathway. Understanding the effect of mmLDL on the ETA receptor and the underlying mechanisms may provide a new idea for the prevention and treatment of cardiovascular diseases.
      PubDate: Wed, 01 Apr 2020 00:50:06 +000
       
  • Attitudes, Opportunities, and Challenges for Clinical Pharmacy Services in
           Mizan-Tepi University Teaching Hospital, Southwest Ethiopia: Health Care
           Providers’ Perspective

    • Abstract: Background. Clinical pharmacy is a branch of health sciences that focuses more on the patient than on drug product-oriented services to optimize drug therapy. This study aimed to assess attitudes, opportunities, and challenges for clinical pharmacy services from the health care providers’ perspective in Mizan-Tepi University Teaching Hospital. Methods. A cross-sectional study was conducted among physicians, nurses, pharmacy professionals, and public health officers working in Mizan-Tepi University Teaching Hospital. A total of 119 health care providers participated in the study, and data were collected using a pretested self-administered questionnaire. The study tool was designed based on the instruments used in the previously conducted studies. Collected data were coded, entered, and analyzed using Statistical Package for the Social Sciences (SPSS, version 21). Furthermore, the descriptive and inferential statistics were performed. Results. Out of 119 health care providers included in the study, 59.66% of them were nurses. The majority of the health care providers (85.71%) had a positive attitude towards clinical pharmacy services. Most of the study participants mentioned that acceptance of clinical pharmacy services among health care providers as a major opportunity to clinical pharmacy services in Mizan-Tepi University Teaching Hospital. The major challenges described for the clinical pharmacy services include lack of support from hospital management, absence of clearly defined roles and responsibilities for the clinical pharmacists, and shortage of pharmacy workforce and staff turnover. Conclusion. Proper strategies should be in place to improve clinical pharmacy services and promote pharmacists’ role in providing patient care.
      PubDate: Tue, 31 Mar 2020 10:05:07 +000
       
  • Acetylation and Evaluation of Taro Boloso-I Starch as Directly
           Compressible Excipient in Tablet Formulation

    • Abstract: Taro Boloso-I (TB1), a newly improved Colocasia esculenta variety, is a potential source of starch with high yield. However, to improve some limitations of the native starches (NS), such as flowability and compactibility, different physical and chemical starch modifications have been employed. Acetylation is one of the chemical modifications which improves the flow and compaction of the NS, which are prerequisite during direct compression (DC) of tablets. Hence, in this study, TB1 starch was acetylated using acetic anhydride and evaluated as an ideal excipient for direct compression. Starch acetates (SA) with a degree of substitution (DS) of 0.072 (SA1) and 0.695 (SA2) were produced and evaluated. FTIR spectra of the SAs were used to verify the acetylation of the NS. Powder flow evaluation parameters showed significant improvement in the flow properties of the NS following acetylation. In addition, the swelling power, solubility, and compactibility were also improved. Tensile strength (TS) of the tablets comprising SAs only, SA1 (41.40) and SA2 (63.43 Kg/cm2), was significantly higher than tablets made of the NS (31.96) and Starch 1500® (15.12 Kg/cm2). The SAs also showed lower sensitivity towards lubrication than the NS and Starch 1500® as lower lubricant sensitivity ratios were recorded. In addition, tablets comprising the SAs satisfactorily accommodated at least up to 50 % w/w paracetamol—compared to 30 % w/w by Starch 1500®—upon DC processing. The paracetamol tablets comprising SAs also complied with the United States Pharmacopeia specifications for disintegration and dissolution studies. Therefore, taking all the facts into consideration, the SAs could be potential DC excipients in tablet formulations.
      PubDate: Thu, 12 Mar 2020 06:20:02 +000
       
  • Physiological and Biochemical Vascular Reactivity Parameters of
           Angiotensin II and the Action of Biased Agonist TRV023

    • Abstract: Vascular reactivity experiments using isolated aortic rings have been widely used as a model for physiological and pharmacological studies since the early sixties. Here, we suggest several parameters that the researcher should pay attention to when investigating angiotensin II in their experimental models. Angiotensin II is one of the active peptides of the renin-angiotensin system and exerts its effect through the AT1 and AT2 receptors. Some studies seek to understand the effects of angiotensin II receptors at the vascular level by using vascular reactivity experiments. However, because of the large number of variations, there are only a handful of reactivity studies that seek to use this method. Thus, the objective of this study was to standardize experimental methods with angiotensin II, through vascular reactivity protocols. For this, variables such as basal tension, concentration interval, single concentration, curve concentration response, and multiple experiments using the same aortic ring were developed using the technique of vascular reactivity in an organ bath. This is the first study that has standardized the vascular reactivity protocol. In addition, we demonstrated the effects of TRV023-biased ligand of the AT1R at vascular sites.
      PubDate: Sun, 01 Mar 2020 00:20:06 +000
       
  • Formulation and Optimization of Monolithic Fixed-Dose Combination of
           Metformin HCl and Glibenclamide Orodispersible Tablets

    • Abstract: The treatment of type II DM involves the use of combination of drugs, especially at the chronic stage. However, the pill burden of this combination therapy combined with swallowing difficulties, occurring at a later stage of DM, has been the major challenge for successful treatment outcomes. This study was aimed at formulating and optimizing a monolithic fixed-dose combination (FDC) of metformin (MET) and glibenclamide (GLB) orodispersible tablets (ODTs) to overcome both the pill burden and swallowing problems. The FDC ODTs were prepared by the melt granulation technique using polyethylene glycol (PEG) 6000 as a binding agent and crospovidone as a superdisintegrant. In the preliminary study, the effects of sodium lauryl sulphate (SLS), PEG 6000, crospovidone, and compression force on friability, disintegration time, and drug release of tablets were investigated. The FT-IR studies showed that there were no incompatibilities between MET and GLB as well as within excipients. The preliminary studies revealed that PEG 6000 and compression force significantly affect both the friability and the disintegration time, while SLS and crospovidone only affect the disintegration time. Therefore, the effects of PEG 6000, crospovidone, and compression force were further studied and optimized using the central composite design. Accordingly, the most desirable optimal values were obtained at 3.82% of PEG 6000, 9.83% of crospovidone, and 10.6 kN compression force having a friability of 0.302% and a disintegration time of 18.7 seconds. From these results, it can be concluded that a monolithic FDC of MET and GLB ODTs having adequate mechanical strength and faster disintegration time was successfully formulated.
      PubDate: Sat, 22 Feb 2020 07:20:02 +000
       
  • Hydroethanolic Stem Bark Extract of Burkea africana Attenuates
           Vincristine-Induced Peripheral Neuropathy in Rats

    • Abstract: Context. The stem bark of the savanna tree Burkea africana (Hook) (family: Leguminosae) is used in the Ghanaian traditional medicine for the management of various pain-related diseases. Objective. This study seeks to investigate the possible antiallodynic and antihyperalgesic effects of the hydroethanolic stem bark extract of B. africana in a vincristine-induced peripheral neuropathy model in rats. Materials and Methods. 0.1 mg kg−1 vincristine was administered intraperitoneally for 5 days followed by 2 days break and continued for another 5 days to establish peripheral neuropathy in Sprague Dawley rats. Effects of Burkea africana extract (BAE) (50–1000 mg kg−1, p.o.) and pregabalin (10–100 mg kg−1, i.p.) were assessed on tactile, intermediate, mechanical, cold, and hot allodynia as well as in the Randall–Sellito test. Moreover, the levels of total proteins, malondialdehyde (MDA), reduced glutathione (GSH), superoxide dismutase (SOD), and catalase (CAT) in sciatic nerve tissue homogenates were assayed. Results. BAE (50–1000 mg kg−1p.o.) showed significant antiallodynic and antihyperalgesic effects similar to pregabalin by increasing paw withdrawal latency and paw withdrawal threshold in all the behavioral tests used. Also, the extract decreased the levels of MDA (a lipid peroxidation product) as well as MPO and caused a significant increase in endogenous antioxidants (GSH) and antioxidant enzymes (SOD and CAT) in tissue homogenates of treated rats. Conclusions. Results from this study indicate that the hydroethanolic stem bark extract of B. africana exhibits antiallodynic and antihyperalgesic effects in vincristine-induced peripheral neuropathy in rats.
      PubDate: Wed, 12 Feb 2020 15:20:06 +000
       
  • Chondrotoxicity of Local Anesthetics: Liposomal Bupivacaine Is Less
           Chondrotoxic than Standard Bupivacaine

    • Abstract: Objective. The purpose of this study is to determine whether (1) liposomal bupivacaine is chondrotoxic; (2) the chondrotoxicity of liposomal bupivacaine differs from standard bupivacaine; and (3) chondrotoxic effects are time dependent. Materials and Methods. We obtained 72 10 mm articular cartilage plugs from 12 fresh bovine distal femoral knee joints and exposed them to either saline, 0.5% bupivacaine, or liposomal bupivacaine for either 30 or 90 minutes. Twenty-four hours after treatment, chondrocyte viability was measured with the use of a fluorescent live/dead assay. An ANOVA test of variance was performed followed by a Holm–Sidak test to make pairwise comparisons across conditions. Student’s t-test was used to compare means. Results. Percent viability of cells exposed to liposomal bupivacaine for 30 minutes was less versus saline control (53.9% ± 21.5% vs. 73.7 ± 18.4%, ), and this remained significant at 90 minutes (49.1% ± 20.3% vs. 67.2% ± 25.6%, ). Liposomal bupivacaine had less chondrotoxic effects when compared with bupivacaine after 90 minutes, with greater viability (49.1% ± 20.3% vs. 21.4% ± 14.0%, ). Chondrotoxicity was found to be time dependent within the bupivacaine group (percent viability at 30 min: 45.5 ± 18.2%, 90 min: 21.4 ± 14.0%, ); however, liposomal bupivacaine did not demonstrate a significant time-dependent chondrotoxic relationship ().Conclusions. Bupivacaine and liposomal bupivacaine are both toxic to chondrocytes. Liposomal bupivacaine is less chondrotoxic than standard bupivacaine and does not demonstrate a time-dependent toxicity.
      PubDate: Sat, 04 Jan 2020 06:20:04 +000
       
 
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