Characterization and ex vivo studies of nanoparticle incorporated transdermal patch of itraconazole

Abstract

Itraconazole, an antifungal drug possess poor solubility, gastrointestinal irritation and first pass effect. Hence in the present work it was initially made as nanoparticles to facilitate absorption and at later stage nanoparticles loaded transdermal patches were developed using promising nanoparticles. Nanoparticles were prepared with Eudragit RL 100 by solvent displacement technique. Formulations F1 to F9 were prepared by using different concentrations of Eudragit RL 100 and polyvinyl alcohol and evaluated for drug content, drug release, entrapment efficiency and mean particle size. The selected formulation was lyophilized to incorporate these formed nanoparticles into transdermal patch by varying concentrations of hydroxy propyl methyl cellulose K100M, polyvinyl alcohol and polyethylene glycol 400. The obtained patches were evaluated for thickness, tensile strength, folding endurance, moisture absorption and moisture content and the drug release showed biphasic release. All the formulations followed first order kinetics, diffusion controlled and fickian release. Flux (ex vivo) studies on rat skin of optimized formulation have high flux of 63.24 μg/cm2/h compared with pure drug, prepared itraconazole ointment 39.15 μg/ cm2/h and prepared itraconazole gel 40.01 μg/cm2/h. The permeability of itraconazole nanoparticle loaded transdermal patch showed 2.63 folds enhancement compared to pure drug. Scanning electron microscopes clearly showed the drug loaded nanoparticle embedment in polymeric transdermal patch. Formulated nanoparticle loaded itraconazole transdermal patch can be successfully used as a carrier for enhancing transdermal permeation and the bioavailability.