Naftifine is used to treat fungal skin infections as it inhibits dermatophytes, which are the cause of onychomycosis. However, naftifine’s ability to permeate the human nail barrier has not been investigated, thus, the antimycotic potential is not clearly established. This work aims to evaluate the effect of penetration enhancing factors on the accumulation of naftifine hydrochloride through human nail clippings. Naftifine polymeric nail lacquers with Eudragit RL100 were developed as a suitable delivery system. Low penetration of naftifine into nail has been determined as less than 10% of applied drug dose accumulated in the nail layers. Incorporation of thioglycolic acid into formulations resulted in increased accumulation of antifungal agent in the nail layers by 100% compared with a control group. Salicylic acid did not effect naftifine accumulation in the human nail. The permeation of naftifine through the nail increased by threefold when the thioglycolic acid-containing formulation was applied and the nail was pretreated with a fractional CO2 laser. Structural changes of the nail barrier, induced by fractional CO2 laser, were visualized by microscopy. The results suggest, that naftifine nail penetration could be significantly increased when physical and chemical enhancing factors are applied.

中文翻译：

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萘替芬用于经甲递送的潜力


萘替芬用于治疗皮肤真菌感染，因为它可以抑制皮肤癣菌，而皮肤癣菌是甲癣的病因。然而，萘替芬渗透人类指甲屏障的能力尚未得到研究，因此，其抗真菌潜力尚未明确。这项工作旨在评估渗透促进因子对盐酸萘替芬通过人体指甲屑积累的影响。含有 Eudragit RL100 的 Naftifine 聚合物指甲油被开发为合适的输送系统。萘替芬对指甲的渗透性较低，已确定为指甲层中累积的药物剂量不到 10%。与对照组相比，在配方中加入巯基乙酸可使指甲层中抗真菌剂的积累增加 100%。水杨酸不会影响萘替芬在人指甲中的积累。当使用含有巯基乙酸的制剂并且用点阵CO2激光预处理指甲时，萘替芬通过指甲的渗透增加了三倍。通过显微镜观察点阵 CO2 激光引起的指甲屏障的结构变化。结果表明，当应用物理和化学增强因子时，萘替芬的指甲渗透力可以显着增加。