FORMULATION AND EVALUATION OF ITRACONAZOLE LOADED CHITOSAN NANOPARTICLES FOR TRANSDERMAL DELIVERY IN CUTANEOUS LEISHMANIASIS
TL;DR
According to the results, itraconazole-loaded nanoparticle transdermal patches made using ionic gelation offer a viable method for enhancing transdermal penetration and bioavailability in antifungal treatment.
Abstract
Itraconazole is a weakly water-soluble antifungal medication whose therapeutic efficacy is diminished by issues such low oral bioavailability, gastrointestinal discomfort, and substantial first-pass metabolism. In order to improve penetration and maintain medication release, this study sought to create and assess itraconazole-loaded nanoparticles using the ionic gelation process and integrate them into a transdermal patch system. Nanoparticles were synthesized utilizing chitosan and sodium tripolyphosphate as cross-linking agents and assessed for particle size, polydispersity index, zeta potential, entrapment efficiency, drug content, and in vitro drug release. The improved formulation demonstrated a particle size of 184 ± 8 nm, a polydispersity index of 0.276, a zeta potential of +28.7 ± 1.5 mV, and an entrapment efficiency of 84.6 ± 1.5%, signifying excellent stability and effective drug encapsulation. The lack of drug-excipient interactions was verified by compatibility investigations. The optimized nanoparticles were lyophilized and added to transdermal patches made with polyvinyl alcohol, polyethylene glycol 400, and hydroxy propyl methyl cellulose K100M. The patches' appropriate thickness, tensile strength, folding durability, moisture absorption, and moisture content were among their good physicochemical characteristics. A sustained biphasic release pattern with 94.2 ± 1.2% drug release over a 24-hour period was demonstrated by in vitro drug release tests. Diffusion-controlled non-Fickian release was indicated by release kinetics that followed first-order and Korsmeyer-Peppas models. In comparison to the pure drug, ex vivo permeation experiments via rat skin showed significantly improved permeation with a flow of 63.24 µg/cm²/h and around 2.63-fold higher permeability. The successful integration of nanoparticles into the polymeric patch matrix was verified by scanning electron microscopy. According to the results, itraconazole-loaded nanoparticle transdermal patches made using ionic gelation offer a viable method for enhancing transdermal penetration and bioavailability in antifungal treatment.