FORMULATION AND CHARACTERIZATION OF ECONAZOLE NITRATE LOADED TRANSFERSOMAL GEL FOR ANTIFUNGAL ACTIVITY

The aim of the present work is to formulate and characterize Econazole nitrate (EN) loaded transfersomal gel for antifungal activity. EN is a broad-spectrum imidazole antifungal agent that belongs to BCS Class II. Due to poor solubility, EN is incompletely absorbed after oral administration and bioavailability vary among individuals. Topical treatment of fungal infections is usually preferred, but the barrier is to cross stratum corneum, so formulating the drug in Transfersomes (TFs) solved this problem. TFs are a highly adaptable, stress-responsive, complex aggregate, and self-regulating membrane. EN loaded transfersomes were prepared by a thin-film hydration method. The EN-loaded transfersomes were optimized by the three factors and two levels Box-Behnken design using Design-Expert software (version 12). Independent formulation variables such as concentrations of phospholipid and two edge activators were evaluated. The prepared TFs were evaluated with respect to particle size, % entrapment efficiency, and % drug release. The prepared EN loaded TFs particle size ranging from 0.28 to 0.71 µm, entrapment efficiency in between 31.5 to 75%, and drug release 80.01 to 95.9%. The optimized F12 TFs batch was formulated by incorporating it into a Carbopol-940 gel base. The EN-loaded transfersomal gel was further evaluated for antifungal activity against Candida albicans. The result showed that the antifungal activity of the EN-loaded TFs was significantly higher than the marketed product (Daktarin^® Gel 2% w/w). Therefore EN loaded transfersomal gel has the ability to penetrate the skin, overcoming the stratum corneum barrier.