Enhancement of tioconazole ungual delivery: Combining nanocapsule formulation and nail poration approaches

Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Fernanda C. Flores, Wing Sin Chiu, Ruy C.R. Beck, Cristiane B. da Silva, M. Begoña Delgado-Charro This work investigated the impact of formulation including in vitro release profile, repeated dosing, and nail poration on the ex vivo nail delivery performance of antifungal formulations. Chitosan coated and uncoated tioconazole-loaded nanocapsules and a nano-based film-forming vehicle were assessed via in vitro release and in vitro permeation tests using an artificial membrane and human nail clippings, respectively. The later involved single and daily dosing experiments with intact and porated nails. Additional experiments with Nile Red-loaded formulations evaluated the depth of penetration of the fluorescent marker into the nail by laser scanning confocal microscopy. The nanocapsule formulations prolonged release of tioconazole for longer than the control solutions and this ability was related to an enhanced nail penetration of the drug. Further, the new film-forming formulation delivered its drug payload more efficiently than a marketed product. Daily dosing of the formulations doubled the amount of drug recovered from the nails. Porating the nails enhanced tioconazole delivery in single dose experiments only. The depth of penetration of Nile Red into the nails clippings ranged between 90–160 μm. This research suggests that ensuring prolonged relea...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research