Formulation and Characterization of Fluconazole as Topical Gel by Porous Microparticle Based Drug Delivery Systems

摘要

Controlled topical release drug delivery system for Fluconazole  is potentially useful in improving drug deposition in the skin and reducing the incidence of adverse side effects. The purpose of the present experiment was to produce a topical gel system for the delivery of . Drug loaded microsponges (1–10) were formulated by an emulsion solvent diffusion method. Optimization of the microsponges was selected by drug loading efficiency. The optimized microsponges was formulated as topical gel and evaluated. The in vitro drug release, ex vivo drug deposition, primary skin irritancy study and in vivo antibacterial activity of  loaded formulations were studied. The spherical and porous microparticles were obtained. Moreover, the optimized microsponge possess particle size, entrapment efficiency and production yield and of 84.49 µm, 72.21% and 39.40% respectively. Microsponge loaded gels indicated controlled release, no irritancy to rat skin and antifungal activity. An in vivo skin deposition study proved three fold higher retention in the stratum corneum layer as compared with plain  gel. Microsponges-based gel formulations showed prolonged efficacy in a rat surgical wound model infected with Candida albicans. These results suggest that was stable in topical formulations and amplifying retention in the skin, indicating better potential of the delivery system for treatment of primary and secondary skin infections. Keywords: Microsponges, Particle size, Entrapment efficiency, Primary skin irritancy, in vivo skin deposition Candida albicans.