The strategy of pharmaceutical innovation has been exploited for enhancing solubility and increased activity to treat fungal and Leishmania infection locally. Various efforts have been carried out to enhance its solubility, however, significant progress was stalled due to less control, instant release, and less stability, which eventually enhanced the formulations’ complications. Renal impairment occurs due to the systemic administration of VRC. VRC is a BCS class-II drug with low solubility and high permeability. Currently, VRC is available for systemic delivery via oral and IV formulation only. Recent studies on fungal and leishmaniasis diseases have demonstrated excellent voriconazole (VRC) efficacy against Candida, Aspergillus, and Leishmania species. Leishmania develops a severe infection of the liver, spleen, and mucocutaneous tissue. Candida infects the mouth, nail, skin, foot, and bloodstream, whereas Aspergillus infects the skin, hair, eyes, and lungs. Candidiasis and Aspergillosis are the most common fungal infections ranging from mucosal and superficial infections to invasive tissue infections. The mortality rate is still high owing to the development of microbial resistance, poor diagnosis, and the limitations of therapy. The development of transethosomal formulation can serve as an efficient drug delivery system through a topical route with enhanced efficacy and better patient compliance.įungal and Leishmania infections are life-threatening to the entire population, especially in immune-compromised patients in underdeveloped countries. 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. Ex-vivo permeation using rat skin depicted a transdermal flux of 22.8 µg/cm 2/h with enhanced efficiency up to 4-fold. 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). 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. The prepared VRCT were evaluated for % yield, % entrapment efficiency (EE), surface morphology, possible chemical interaction, particle size, zeta potential, and polydispersity index (PDI). We herein report voriconazole-loaded transethosomes (VRCT) fabricated by the cold method and followed by their incorporation into carbopol 940 as a gel. Transethosomes (TELs) are one of the potential innovative nano-carriers for improving the solubility and permeation of poorly soluble and permeable drugs. Despite many efforts to enhance its solubility, this primary issue still remains challenging for formulation scientists. Voriconazole (VRC) is a broad-spectrum antifungal agent belonging to BCS class II (biopharmaceutical classification system).
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