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1.
Molecules ; 27(10)2022 May 23.
Artículo en Inglés | MEDLINE | ID: mdl-35630825

RESUMEN

Voriconazole (VRC) is a broad-spectrum antifungal agent belonging to BCS class II (biopharmaceutical classification system). Despite many efforts to enhance its solubility, this primary issue still remains challenging for formulation scientists. Transethosomes (TELs) are one of the potential innovative nano-carriers for improving the solubility and permeation of poorly soluble and permeable drugs. We herein report voriconazole-loaded transethosomes (VRCT) fabricated by the cold method and followed by their incorporation into carbopol 940 as a gel. The prepared VRCT were evaluated for % yield, % entrapment efficiency (EE), surface morphology, possible chemical interaction, particle size, zeta potential, and polydispersity index (PDI). The optimized formulation had a particle size of 228.2 nm, a zeta potential of -26.5 mV, and a PDI of 0.45 with enhanced % EE. Rheology, spreadability, extrudability, in vitro release, skin permeation, molecular docking, antifungal, and antileishmanial activity were also assessed for VRCT and VRC loaded transethosomal gel (VTEG). Ex-vivo permeation using rat skin depicted a transdermal flux of 22.8 µg/cm2/h with enhanced efficiency up to 4-fold. A two-fold reduction in inhibitory as well as fungicidal concentration was observed against various fungal strains by VRCT and VTEG besides similar results against L-donovani. The development of transethosomal formulation can serve as an efficient drug delivery system through a topical route with enhanced efficacy and better patient compliance.


Asunto(s)
Antifúngicos , Antiprotozoarios , Animales , Antifúngicos/farmacología , Antiprotozoarios/farmacología , Portadores de Fármacos/química , Simulación del Acoplamiento Molecular , Ratas , Absorción Cutánea , Voriconazol/farmacología
2.
Pak J Pharm Sci ; 35(6): 1573-1580, 2022 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-36789817

RESUMEN

The main objective of this study to formulate of fast dissolving tablets of sofosbuvir, an antiviral drug used for hepatitis C virus. The direct compression method was employed for the formulation of sofosbuvir FDT and optimized for weight variation test, thickness, hardness, friability, wetting time, water absorption ratio, in-vitro disintegration test, and in-vitro dissolution studies, assay identification by using HPLC and stability studies. Master formulation of F4, Sofosbuvir showed promising results compared to others formulations and selected as the most suitable and best formulation among them. It also has better efficacy, disintegration and dissolution time. F4 was fabricated with both super disintegrants like croscarmellose sodium and sodium starch glycolate that lead to its required features. This formulation would be a good alternate for the management of viral diseases with better dissolution profile, stability and improved bioavailability for the patients.


Asunto(s)
Química Farmacéutica , Sofosbuvir , Humanos , Química Farmacéutica/métodos , Antivirales , Solubilidad , Excipientes , Comprimidos
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