盐酸特比萘芬醇类脂泡囊凝胶离体和在体透皮特点研究

Study on the Transdermal Characteristics of Terbinafinol Hydrochloride Alcohol Lipid Vesicles Gels in vitro and in vivo

目的:研究盐酸特比萘芬醇类脂泡囊凝胶在体和离体透皮特点。方法:采用Franz扩散池进行体外透皮实验,考察盐酸特比萘芬醇类脂泡囊凝胶、脂质体凝胶和普通凝胶经皮渗透性和皮肤滞留量;以小鼠为实验动物,3种凝胶腹部经皮给药,考察盐酸特比萘芬的血药浓度和皮肤滞留量,对比不同类型凝胶剂的透皮效果。结果:离体透皮扩散实验中,透皮速率排序为:脂质体凝胶>醇类脂泡囊凝胶>普通凝胶;皮肤内24 h累积滞留量排序为:醇类脂泡囊凝胶>脂质体凝胶>普通凝胶。在体透皮吸收实验中,皮肤内6 h累积滞留量排序为:醇类脂泡囊凝胶>脂质体凝胶>普通凝胶。3种凝胶中的盐酸特比萘芬在皮肤深层中的滞留量均远远大于角质层,醇类脂泡囊凝胶中药物在皮肤深层的滞留量远大于另外两种凝胶,而脂质体凝胶和普通凝胶在皮肤深层的滞留量无明显差异。结论:醇类脂泡囊对盐酸特比萘芬透皮吸收具有一定的促进作用,同时也能显著提高盐酸特比萘芬在皮肤内特别是皮肤深层中的滞留量,为治疗深部皮肤真菌感染提供了一种新方法。

Objective:To study the transdermal characteristics of terbinafenafenol hydrochloride lipovesicular gels in vitro and in vivo.Methods:Tebinafine hydrochloride alcohol lipid vesicles gel,liposome gel and normal gel were respectively prepared.In vitro transdermal experiments were carried out on mouse skin in Franz diffusion cells to investigate the transdermal permeability and skin retention.Mice were used as the experimental animals and given medicine on abdominal skin.Blood was collected and skin was withdrawn regularly.The blood drug concentration and skin drug retention were investigated,and the transdermal effects of different types of gels was compared.Results:In the in vitro transdermal diffusion test,the transdermal rate was ranked as liposome gel>alcohol lipid vesicles gel>normal gel.The cumulative hysteresis of 24 h in skin was sorted as alcohol lipid vesicles gel>liposome gel>normal gel.In the body transdermal absorption test,the accumulated hysteresis of 6 h in skin was sorted as alcohol lipid vesicles gel>liposome gel>normal gel.In the three gels,the hysteresis in the deep layer of skin was much more than that in the cuticle,and the hysteresis of the alcohol follicle gel was much more than that of the other two gels.There was no significant difference between liposome gel and ordinary gel in the deep layer of skin.Conclusion:Alcohol lipid vesicles have a certain effect on the transdermal absorption of terbinaphthalene hydrochloride.At the same time,it can significantly increase the retention of terbinaphthalene hydrochloride in skin,especially in the deep skin,which provides a new method for the treatment of deep skin fungal infections.