Investigation Of Formulation Variables In The Design And Development Of Voriconazole Bilosomes

Abstract

Voriconazole is a synthetic, second-generation, broad-spectrum triazole derivative of fluconazole that disrupts the cell membrane and stops fungal growth by inhibiting the cytochrome P450 (CYP) dependent enzyme 14-α-sterol demethylase. Bilosomes are non-ionic, amphilic, flexible surfactant delivery vehicles, which contain bile salts to improve oral and skin delivery of drugs at various doses. This study aims to prepare Voriconazole bilosomes as vesicular carriers and assess the effect of different formulation variables such as type and amount of surfactant, amount of cholesterol, amount of bile salts, and sonication time on particle size, entrapment efficiency, and polydispersity index of the prepared bilosomes. The bilosomes were prepared by thin film hydration method and they were optimized using different types of non-ionic surfactants span80 and Tween80 along with different amounts of cholesterol and different sonication times. The objective was to administer voriconazole sustained-release formulation once daily for a whole day to attain an ideal release profile