TRANSUNGUAL PERMEATION OF THE VORICONAZOLE NAIL LACQUER AGAINST TRICHOPHYTON RUBRUM

Abstract

Introduction: The oral therapies encounter side effects and topical therapies for nail diseases are limited by poor permeability of nail plate. An optimal penetration enhancer would improve drug delivery through nail plate facilitating new possibilities for treating neighboring target sites if the systemic circulation is reached. The purpose of study was to determine amount of voriconazole permeating through the nail plate from the nail lacquer formulation containing permeation enhancer and to demonstrate its susceptibility to the onchomycotic dermatophyte. Methods and materials: The permeability studies were performed on avulsed human cadaver nail plates using modified Franz diffusion apparatus containing phosphate buffer saline in the acceptor chamber. The amount of Voriconazole permeated was quantitatively determined by the UV spectrophotometer. The amount of Voriconazole remaining in the nail after permeation had been retrieved by milling test. Results and discussion: The addition of thioglycolic acid, 5% improved the permeability of the drug by 0.7 as the enhancement factor. The formulation followed zero order kinetics and Korsmeyer- Peppas mechanism of drug release on analyzing on DDSolver. The voriconazole flux of 5592.1 µg/cm/min and 596.75 µg/cm/min had been observed at 24 and 48 hours aliquots respectively for the nail lacquer containing an enhancer. Significantly higher permeation rates were achieved in the presence of an enhancer. Conclusion: The inhibitory zones for the voriconazole transungual nail lacquer were evaluated by testing against the dermatophyte, Trichophyton rubrum on Sabouraud’s Dextrose Agar. The effective zones of inhibitions suggested Voriconazole nail lacquer exhibiting moderate antifungal activity for the onchomycosis treatment.