The results were further confirmed by different pharmacokinetic parameters-it was observed that the developed optimized floating ATS spheroid-loaded NLCs formulation has significantly improved relative bioavailability, that is, 3.053-folds through oral route in comparison to marketed formulation.
Orally administered pharmaceuticals now account for 74% of all prescriptions, however studies have shown that oral medications are often less effective due to first pass metabolism and not stable drug blood level etc. Transdermal drug delivery system (TDDS) was developed to enhance such qualities. Every 2.2 years, the FDA grants approval for a new transdermal medication delivery system, fueling a multibillion dollar industry. An extensive evaluation of the technology, business, and products has been warranted since the FDA initially authorized the first transdermal medicine patch around 40 years ago. Transdermal medication delivery systems on demand are made possible by patches, a special kind of patch. The transdermal medication delivery system's adhesive plays a key role in the product's safety, effectiveness, and quality. Compared to more traditional delivery modalities, such as oral or invasive injection, topical therapy provides several benefits. Limiting hepatic first-pass metabolism, improving therapeutic efficacy, and maintaining a constant plasma level are all benefits of transdermal drug administration. Types of transdermal patches, production techniques, mechanism of action, kinetics, clinical concerns, and their physicochemical methods of assessment are all covered in this article.
Objective: The aim of present investigation is docking of various existing antiviral, anti-tubercular and anti-malarial drugs on 6LU7 receptor of SARS-CoV-2 in the treatment of COVID-19. Methods: In this study, the structure of coronavirus binding protein and ligands for various drugs were collected from the protein data bank and pub chem. Molecular docking was carried out using Schrodinger 9.0 software. In molecular docking study, 19 different drugs of various categories like antiviral, anti-malarial and anti-tubercular were investigated for analyzing binding to 6LU7 receptors of COVID-19. Results: The docking result showed a high affinity of zanamivir, montelukast, ramdesvir, ritonavir, cobicistat and favipravir to the 6LU7 receptor of novel coronavirus. Thus the combination of these drugs may be useful in preventing further infection and can be used as a potential target for further in vitro and in vivo studies of SARS-CoV-2. Conclusion: Treatment of COVID-19 has been challenge due to the non-availability of effective drug therapy. In this study, we reported drugs for targeting 6LU7 Mpro/3Clpro protein, which showed prominent effects as potential inhibitors of COVID-19 Mpro.
Objective: Development and evaluation of self-emulsified drug delivery system of embelin for the treatment of amoebiasis. Methods: Self-emulsifying drug delivery systems (SEDDS) were prepared by determining the saturation solubility of embelin in different oil, surfactant and co-surfactant. Pseudo-ternary phase diagram was prepared by using chemix software for the selection of surfactant and co-surfactant ratio, and was optimized as 2:1 (Surfactant: Co-surfactant) for SEDDS. The drug was dissolved in surfactant, followed by the addition of co-surfactant and oil in a beaker. The resultant mixtures were stirred continuously by magnetic stirrer and heated at 40 °C to obtain a homogenous mixture. The prepared drug-loaded SEDD formulation was optimized on the basis of emulsification time, size, PDI, zeta potential and precipitation of drugs. Then the anti-amoebic activity of embelin and metronidazole-loaded SEDDS powder was carried out using microplate reader. Results: The optimum solubility of embelin was calculated in Capmul MCM EP as oil (37 mg/ml), Kolliphor hs 15 as surfactant (150 mg/ml) and PEG 400 as co-surfactant (19 mg/ml). The formulation F7 i.e. 70% Smix and 30% oil was estimated as optimized formulation. The different values of emblein loaded SEDDS was found to be dilution test (no sign of precipitation), centrifugation test (no sign of phase separation), globule size (Dia 217.5 nm) and PDI (108), zeta potential determination (-31.60 mV), viscosity (17.12 cps) and Eosin red confirmed the o/w type of emulsion. Moreover, the angle of repose SEDDS prepared by using Avicel 200 was found to be Θ=27.474, means flow of powder is good with drug loading capacity of 92.7 %. SEM image and in vitro drug release indicated the 99.3% drug was released from the SEDDS in 120 min. Cytotoxicity study (MTT assay) shows the Plain Drug Suspension, Embelin loaded SEDDS powder and Metronidazole exhibited 100% viability at the concentration range of 1.56-100 mmol. The anti-amoebic IC50 values of embelin, metronidazole and embelin loaded SEDDS powder was found 1.519 µmol, 1.354 µmol, 1.84 µmol and 1.35 µmol, respectively. Conclusion: Present study showed the stronger amoebicidal action of embelin may associated with some specific interaction of the active embelin with the cell wall of the parasites or with a more effective mechanism of penetration into the parasites through membrane channels.
Objective: Desіgn anԁ Evаluаtіon of Olаnzаpіne anԁ Rіsperіԁone Trаnsԁermаl Pаtches Methodology: Usіng blenԁs of two ԁіfferent polymerіc combіnаtіons, Euԁrаgіt RL 100 (ERL 100) аnԁ Euԁrаgіt (ERS 100). А totаl of twenty-two mаtrіx pаtches were prepаreԁ by usіng these polymers, surfаctаnts (cаtіonіc surfаctаnt, benzаlkonіum chlorіԁe (BC); аnіonіc surfаctаnt, soԁіum lаuryl sulphаte (SLS); non-іonіc surfаctаnt, spаn 20) аnԁ vegetаble oіls (olіve oіl, jojobа oіl аnԁ grounԁnut oіl) аs permeаtіon enhаncers іn іsopropаnol-ԁіchloromethаne (60:40) аs а solvent system. The formulаtіons were chаrаcterіzeԁіncluԁіng unіformіty of weіght, ԁrug content, moіsture content, moіsture uptаke, flаtness, folԁіng enԁurаnce аnԁ thіckness to stuԁy the stаbіlіty of the formulаtіons аnԁіn vіtro ԁіssolutіon of the experіmentаl formulаtіons were performeԁ to ԁetermіne the аmount of Olаnzаpіne аnԁ Rіsperіԁone present іn the pаtches аnԁ scаnnіng electron mіcroscopy (SEM) of the prepаreԁ TԁԁS were tаken to see the ԁrug ԁіstrіbutіon pаttern. ԁrug–excіpіent іnterаctіon stuԁіes were cаrrіeԁ out usіng Fourіer trаnsform іnfrаreԁ (FTІR) spectroscopіc technіque. Results: Іn vіtro ԁіssolutіon stuԁіes showeԁ thаt the ԁrug ԁіstrіbutіon іn the mаtrіx wаs homogeneous аnԁ іt wаs founԁ thаt the mаxіmum ԁrug releаse аnԁ іn stаbіlіty stuԁy ԁrug content wаs founԁ to be 97.03%, 97.02% аnԁ 96.32% аfter 1, 2 аnԁ 3 months respectіvely wіth formulаtіon ROE3 (contаіnіng olіve oіl). Іn vіtro skіn permeаtіon stuԁy wаs аlso conԁucteԁ іn а moԁіfіeԁ Frаnz's ԁіffusіon cell whіch shows thаt the mаxіmum permeаtіon wаs wіth the formulаtіon ROE3 аnԁ іt wаs mаxіmum trаnsԁermаl flux 23.14 μg/cm2/h wаs obtаіneԁ wіth formulаtіon contаіnіng olіve oіl аs permeаtіon enhаncer respectіvely. Conclusions: Optіmіzeԁ formulаtіons were founԁ to be suіtаble for formulаtіng іn terms of physіcochemіcаl chаrаcterіstіcs аnԁ there wаs no sіgnіfіcаnt іnterаctіon notіceԁ between the ԁrug аnԁ polymers useԁ.
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