Formulation of gel containing clotrimazole-loaded nanoparticles

Abstract

Background: Clotrimazole (CLO) is an imidazole derivative with antifungal activities. The conventional dosage forms for oral or topical administration have some disadvantages such as drug adverse reaction for long-term use, repeated doses daily due to short half-life. The aim of this study was to prepare gel containing CLO-loaded nanoparticles to increase drug solubility, enhance bioavailability, especially for a sustained drug release. Materials and methods: Eudragit RS 100 nanoparticles were prepared by the nanoprecipitation method, then was mixed with gel forming excipient. Gel containing CLO-loaded nanoparticles was characterized in terms of appearance, pH, particle size, PDI, encapsulation efficiency (EE), in vitro drug release. Results: The best formulation of gel containing 1% of CLO-loaded nanoparticles with 0.3% of Carbopol 934P, 5% of glycerin was smooth, homogenous, and particle size, PDI, EE, drug release of 154.6 ± 3.6 nm, 0.153 ± 0.011, 67.62 ± 0.89%, 51.46 ± 1.10% (after 24 hours). Conclusion: Gel containing CLO-loaded nanoparticles is a promising drug delivery system for the topical treatment of fungal infections. Key words: clotrimazole, Eudragit RS 100, fungal infection, nanoparticle, topical treatment