<p>Clotrimazole is poorly soluble synthetic, azole antifungal derivative which is used in treatment of fungal infections. This study aimed to formulate and optimize nanoemulgel to improve solubility and permeation of clotrimazole. The clotrimazole nanoemulgel was prepared by aqueous titration–probe sonication method and optimized by three levels–three factors Box–Behnken design. At 100&#xa0;rpm, the optimum viscosity was 1134.8 Cp. Transmission electron microscopy (nano range), zeta potential (− 11.5&#xa0;mV), globule size (355.3&#xa0;nm with PDI 0.464), drug content (93 ± 0.28%) and rheological characteristics (pH 6.21 and Refractive Index 1.433) are all desirable. Franz diffusion cell was used for the permeation investigation, and the results showed that 83.61% of the drug permeation and enhancement factor (3.16) was good when compared to the marketed formulation (2.61). In comparison to the clotrimazole and commercial preparation, it exhibits 2.42 times greater in vitro antifungal activity against <i>Aspergillus niger</i> and causes no skin irritation in the skin of Wistar Albino rats. It can be concluded that topical administration of clotrimazole nanoemulgel increases the solubility, permeability, and diffusibility of the drug with enhanced antifungal activity.</p>

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Nanoemulgel for Treatment of Topical Fungal Infection: Formulation and Optimization Using Box–Behnken Design

  • Raksha Laxman Mhetre,
  • Aditee Deepak Kagade,
  • Shashikant N. Dhole

摘要

Clotrimazole is poorly soluble synthetic, azole antifungal derivative which is used in treatment of fungal infections. This study aimed to formulate and optimize nanoemulgel to improve solubility and permeation of clotrimazole. The clotrimazole nanoemulgel was prepared by aqueous titration–probe sonication method and optimized by three levels–three factors Box–Behnken design. At 100 rpm, the optimum viscosity was 1134.8 Cp. Transmission electron microscopy (nano range), zeta potential (− 11.5 mV), globule size (355.3 nm with PDI 0.464), drug content (93 ± 0.28%) and rheological characteristics (pH 6.21 and Refractive Index 1.433) are all desirable. Franz diffusion cell was used for the permeation investigation, and the results showed that 83.61% of the drug permeation and enhancement factor (3.16) was good when compared to the marketed formulation (2.61). In comparison to the clotrimazole and commercial preparation, it exhibits 2.42 times greater in vitro antifungal activity against Aspergillus niger and causes no skin irritation in the skin of Wistar Albino rats. It can be concluded that topical administration of clotrimazole nanoemulgel increases the solubility, permeability, and diffusibility of the drug with enhanced antifungal activity.