科研之友
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摘要
The objective was to prepare a novel nail lacquer formulation to improve the ungual and trans-ungual delivery of apremilast for the potential treatment of nail psoriasis. Nail lacquer formulation was prepared using EudragitA (R) S 100 as a film-forming polymer and the mixture of ethanol, ethyl acetate, and water as a solvent system. As a result of high-throughput screening studies, dexpanthenol and salicylic acid were found to be the potential penetration enhancers. After 7 days of in vitro studies, the cumulative amount of apremilast delivered by the nail lacquer formulation across the nail plate was found to be similar to 3-fold (0.52 +/- 0.07 mu g/cm(2)) more compared to control (nail lacquer formulation without enhancers) (0.19 +/- 0.02 mu g/cm(2)). The cumulative amount of apremilast retained in the nail plate in the case of nail lacquer formulation was 1.26 +/- 0.18 mu g/mg which was found to be similar to 2-fold more compared to control (0.57 +/- 0.07 mu g/mg). Human subject studies were performed on the nails of thumb and index finger of six volunteers for 15 days. As a result, the cumulative amount of apremilast retained in the free distal edge of the nail plate in the case of nail lacquer was found to be similar to 2-fold (0.93 +/- 0.14 mu g/mg) more related to control (0.41 +/- 0.04 mu g/mg). As a conclusion, nail lacquer formulation was found to be capable of delivering a substantial amount of apremilast into the nail apparatus; thus, it can be a potential option for the treatment of nail psoriasis.
- 出版日期2017-11
