Posted by admin on Jul 31, 2023 in |
Staphylococcus aureusis a Gram-positive facultative pathogenic bacterium responsible for a wide range of infections ranging from skin to life-threatening infections. Antibiotic resistance of Staphylococcus aureus is an emerging global concern. Thus, developing viable antibiotics are in high demand. This study identified novel lead compounds from traditionally used medicinal plants via in-silico molecular docking and in-vitro antibacterial analysis. Thus, we have derived literature-evident phytocompounds from numerous traditional medicinal plants such as Boerhavia diffusa, Clerodendrum infortunatum, Sida rhombifolia, Tephrosia purpurea, Scoparia dulcis, Breynia retusa, Euphorbia heterophylla, Hemigraphis alternata, Hedyotis corymbose, Imperata cylindrica and their structures were retrieved from PubChem. Lipinski’s rule in ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity) profiles were used to screen derived phytocompounds, followed by in-silico docking to the target protein. Clumping factor A (ClfA)-fibrinogen, a key virulence factor in S. aureus, was taken as a target protein. ClfA is a cell-wall-anchored protein that causes bacterial adherence to the blood plasma protein fibrinogen, which causes a variety of infections. Thus, an appealing strategy is to discover a novel lead compound with...
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Posted by admin on Jul 31, 2023 in |
The primary goal of this study was to evaluate solid lipids as an alternative to polymers in the formulation of oral modified-release pastilles. Lipids have been used in pharmaceuticals since ancient times for a variety of purposes. They are used as polymer substitutes in the development of dosage forms. The solvent-free technique of pastillation uses lipids to formulate a modified-release oral dosage form explored in this research study. The melt solidification apparatus was developed at the laboratory scale to formulate hemispherical-shaped pastilles using solid lipid stearic acid; the apparatus was optimized by applying a 23-factorial design in Minitab. Three factors (X1 needle gage, X2 dropping height, and X3 base plate temperature) were considered and studied at 2-level.Optimized conditions were found to be ideal dropping height of 1 cm, a needle gauge of 20 G, and a cooling plate temperature of 4°C. Pastilles were characterized for drug content uniformity, 94 ± 1.64% to 98.8 ±1.03%; drug release of the F8 batch showed 99.98% ± 1.09 drug release at 12 hr;...
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Posted by admin on Jul 31, 2023 in |
Moxifloxacin (MOX) is a second-line treatment for drug-susceptible and multidrug-resistant tuberculosis (MDR TB). MOX has poor patient compliance due to taste and odour concerns, particularly in the pediatric population. MOX taste-masked chewable tablets were developed by direct compression method using mannitol, aspartame, and sucralose as sweetening agents and lemon and peppermint flavor as flavoring agents. The lubricated granules were evaluated for flow properties, and compressed tablets were evaluated for hardness, friability, content uniformity, weight variation, DT and in-vitro drug release. FTIR, DSC, and XRD analysis were performed to detect any possible drug excipient compatibility issues and the nature of the drug molecule in the formulation. F6 formulation granules showed excellent flow properties, and batches manufactured with these granules showed physicochemical properties within acceptable limits. Complete drug release was observed within 8 minutes from the F6 formulation. FTIR and DSC studies demonstrated no drug excipient compatibility issues. According to XRD, the MOX in the final formulation was present in crystalline form. The dispersible MOX pills would be a superior alternative...
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Posted by admin on Jul 31, 2023 in |
Nowadays, the use of herbal drugs is tremendously increased due to the lesser number of side effects when compared to pure form of drugs. Herbal medicine is a complex compound with multiple synergistic mechanisms of action which modulate pathophysiological functions. Even though few herbs exhibit toxicity, they possess many therapeutic values and curative principles; one such herb is calotropis. It exists in three species that produce pharmacological effects: cardiovascular, anti-cancer, antimicrobial, anticonvulsant, and smooth muscle relaxant. In this research, 24 chemical constituents of all calotropis species were selected. The molecular properties, bioactivity scores, ADMET profile of 24 calotropis species chemical constituents were predicted using computational tools, including mol inspiration, Pre ADMET, and structures drawn using chem sketch. The results drawn from the study were compounds C8[Syriogenin] and C16[urosolic acid] exhibited good oral bioavailability, bioactivity scores, intestinal absorption, renal absorption, decreased metabolism rate by inhibiting CYP3A4 and less toxic by Ames...
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Posted by admin on Jul 31, 2023 in |
The Bionanofibers drug delivery systems can reduce toxicity, improve therapeutic efficacy and increase patient compliance by delivering drugs at a controlled rate to the site of action. The major aim in designing nanostructures as delivery systems is to deliver pharmacologically active molecules with accurate doses at targeted sites. The present research work developed Bionanofibers as a carrier for drug delivery. Because of the very small nanoscale diameter and high surface area, significantly higher drug content can be loaded in a very small volume. Bionanofibers were manufactured from Macitentan drug using PVP and Soybean PC by electrospinning. The obtained bionanofibers were characterized based on morphology, entrapment efficiency, and drug release behavior. FE-SEM images showed that the length of obtained bionanofibers is about 580nm to 1250nm in diameter. FTIR analysis shows no significant interaction between the drug and the polymer. The in-vitro release study demonstrated that there is a controlled release pattern of drugs from...
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