FORMULATION AND EVALUATION OF ITRACONAZOLE NIOSOMAL GEL FOR TOPICAL APPLICATION

Itraconazole is a broad spectrum Imidazole derivative useful in the treatment of superfacial and systemic fungal infection. The present study was to formulate and evaluate the Itraconazole niosomal gel using surfactant span 40, 60 and tween 60 for the preparation of niosomes. The main objective of the study was to enhance the antifungal activity of the formulation. Itraconazole niosomes were prepared by thin film hydration method using span 40, 60 and tween 60 (as non-ionic surfactant) and cholesterol (as stable vesicle forming agent). Niosomes were prepared using different ratio of drug: surfactant: cholesterol (1:1:0.2, 1:1.5:0.3, 1:2:0.4). The niosomal dispersion was evaluated for vesicle size, surface morphology, percent entrapment efficiency, drug content and in vitro drug release. The entrapment efficiency and drug content were calculated at 262 nm using UV spectrophotometer. The entrapment efficiency was found to be 71.2%, 62.2% and 59.2% for the formulations F5, F7 and F6. Itraconazole niosomal gel was prepared using Carbopol 940, glycerol, triethanolamine and distilled water. Evaluation of niosomal gel was determined by physical appearance, pH, viscosity, drug content, entrapment efficiency and In-vitro permeation studies. The percentage of the drug release from the niosomal gel was found to be 98.87% for FG-2 after 24 hrs. The present study demonstrates prolongation of drug release, an increase in amount of drug retention into skin and improved permeation across the skin after encapsulation of Itraconazole into niosomal topical gel.

Keywords: Itraconazole, Niosomes, Fungal infection, Thin film hydration method, Carbopol 940.