Formulation and Evaluation of Itraconazole Niosomal Gel for Topical Application
Niosomes have potential applications in topical drug delivery system. Niosomes play an increasingly important role in drug delivery as they can reduce toxicity and modify pharmacokinetic and bio-availability. Topically applied niosomes can increase the residence time of drugs in the stratum corneum and epidermis, while reducing the systemic absorption of the drug. It can act as drug containing reservoirs and the modification of the vesicular compositions or surface properties can adjust the drug release rate and the affinity for the target site. Itraconazole is a triazole derivative useful in the treatment of number of fungal infections. This includes aspergillosis, blastomycosis, coccidioidomycosis, histoplasmosis, and paracoccidioidomycosis. It may be given by mouth or intravenously. Itraconazole niosomes were prepared by thin film hydration method using span 20, 40, 60 (as non-ionic surfactant) and cholesterol (as stable vesicle forming agent). Niosomes were prepared using different ratio of drug: surfactant: cholesterol (1:1:1, 1:2:1, 1:3:1). 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 57.2%, 73.2% and 61.2% for the formulations ITZ 20-3, ITZ 40-2 and ITZ 60-1. 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 55.67 % for ITZG-2. 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: Niosomes, Itraconazole, Fungal infection, Thin film hydration method, Carbopol 940
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