Development and Evaluation of Antifungal Efficacy of Ketoconazole Pharmacosome

Abstract

Pharmacosomes are neutral colloidal, lipid vesicular drug delivery system having both negative & positive charge that enhance the bioavailability of drugs by enhacing their solubility both in aqueous as well as non-aqueous phase, additionally reduce gastrointestinal toxicity of drug. Ketoconazole is an imidazole derivative agent which is used both in the treatment of topical or systematic fungal infections with fungi static activity against dermatophytes, yeasts and other pathogenic fungi. Ketoconazole is Biopharmaceutical classification system (BCS) class II drugs that display pH dependent dissolution and absorption. In this present research work Pharmacosome of Ketoconazole was prepared in different ratios of Ketoconazole-PC complex (1:1, 1:1.5 and1:2) using conventional solvent evaporation method. FT-IR spectra showed no significant untoward interaction, Vesicles shape and morphology was carried out with Phase contrast microscopy (PCM) and Scanning electron microscopy (SEM), In-vitro permeation study and anti-fungal activity were duly examined. Drug content in the formulations (1:1) (1:1.5) and (1:2) were found 92.5%, 94.3% and 89.7% respectively. FT-IR conformed proper formation of drug- Pharmaosome complex. Particle size distribution were found to be regular and of spherical shape. In-vitro permeation study showed 78.03%, 89.05% and 55.27% drug release as per respectively formulations (KTP1, KTP2 and KTP3). Pharmacosomes of ketoconazole show improvement in antifungal activity than ketoconazole (Pure).