Department of Clinical Pharmacy, Lithuanian University of Health Sciences, Sukilėlių pr. 13, Kaunas 50161, Lithuania.
Institute of Pharmaceutical Technologies, Lithuanian University of Health Sciences, Sukilėlių pr. 13, Kaunas 50161, Lithuania.
Molecules. 2020 Jul 3;25(13):3043. doi: 10.3390/molecules25133043.
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 CO laser. Structural changes of the nail barrier, induced by fractional CO laser, were visualized by microscopy. The results suggest, that naftifine nail penetration could be significantly increased when physical and chemical enhancing factors are applied.
萘替芬用于治疗真菌感染,因为它可以抑制皮肤癣菌,而皮肤癣菌是甲真菌病的病因。然而,尚未研究萘替芬穿透人体指甲屏障的能力,因此其抗真菌潜力尚不清楚。本工作旨在评估渗透增强因子对盐酸萘替芬通过人指甲屑积累的影响。开发了含有 Eudragit RL100 的萘替芬聚合物指甲漆作为合适的递送系统。已经确定,萘替芬在指甲中的低渗透性小于应用于指甲层的药物剂量的 10%。与对照组相比,将巯基乙酸掺入制剂中可使抗真菌剂在指甲层中的积累增加 100%。水杨酸对人指甲中萘替芬的积累没有影响。当应用含有巯基乙酸的制剂并对指甲进行分束 CO2 激光预处理时,萘替芬通过指甲的渗透增加了三倍。分束 CO2 激光诱导的指甲屏障的结构变化通过显微镜可视化。结果表明,当应用物理和化学增强因子时,萘替芬指甲渗透可以显著增加。