Fabrication and characterization of film-forming voriconazole transdermal spray for the treatment of fungal infection

Abstract

Voriconazole is second-generation triazole used for the treatment of fungal infections but has serious unwanted adverse effects, which could be reduced by topical semisolid dosage form. Major drawbacks of topical semisolid products are poor patient compliance, cross contamination; gels are easily rubbed off by clothing and during day-to-day activities, physical instability. The purpose of the present work was to fabricate 0.5% w/w voriconazole transdermal spray for fungal infection. The transdermal spray was generated by using a film forming polymers like Eudragit RLPO and ethyl cellulose (1:2 ratios) along with eutectic camphor: menthol (1:1) mixture used as a penetration enhancer. The formulation optimized by constrained 3² factorial design. Regression analysis and response surface methodology were used to optimize the effect of polymers and formulate checkpoint batch based on overlay plots. The transdermal spray was subjected to evaluate parameters related to formulation and containers. The concentration of Eudragit RLPO and ethyl cellulose was showed influence on viscosity as well as t₅₀. Diffusion study was showed 75% of voriconazole transport with 65.8 μgcm⁻² h⁻¹ fluxes. Penetration enhancers’ had shown an increase in 1.68 fold of the penetration of voriconazole through the formulation. The study was concluded that fabricated film forming voriconazole transdermal spray formulations penetrate to the deep layer of the skin and was feasible to treat the dermatological fungal infection. This delivery platform is opened a wide range of treatment of fungal infection as compared to conventional formulations.