FORMULATION AND EVALUATION OF TOPICAL CUBOSOMAL EMULGEL OF AN ANTIFUNGAL DRUG: ITRACONAZOLE

Abstract

An antifungal drug Itraconazole is an azole derivative that belongs to BCS class II. Itraconazole with 14-α demethylase, a cytochrome P-450 enzyme obligatory to convert lanosterol to ergosterol; as ergosterol is an imperative component of the fungal cell wall. The present research work aims to extend the penetration of Itraconazole into deeper layers of skin by formulating cubosomes of Itraconazole into a topical emulgel that helps in enhancing the bioavailability by avoiding first-pass metabolism. Cubosomes were prepared by the Top-down approach (Emulsification method) employing GMO as a lipid phase vehicle, Pluronic F127 as a stabilizer, and distilled water as the aqueous phase. Itraconazole is an antifungal drug with 55% oral bioavailability. Consequential formulations were characterized by visual inspection, encapsulation efficiency, in-vitro drug release, particle size, zeta potential. Optimized formulation (F4) showed drug release of 89.76% within 9 hours, the particle size of 259.8 d.nm, and zeta potential of -34.4 mV. The optimized Cubosome formulation F4 was used for the Itraconazole emulgel using carbopol 974N, HPMC 15cps, and studied for pH, viscosity, drug content and in vitro drug release. Among all the preparations, formulation ITF7 was found to illustrate the utmost drug release of 86.93% at the closing stages of 20 hours and other evaluation parameters within specified limits. In vitro release kinetics exhibited sustained release and therefore the formulation ITF7 follows the Higuchi release mechanism and according to this model, the Itraconazole cubosomal emulgel formulation released the drug throughout non-Fickian super case-II transport (n > 0.89). This novel cubosomal, low-irritant gel would be a promising system for effectual topical drug delivery.