丙二醇-肉豆蔻酸异丙酯系统中促透剂对来曲唑经皮透过性的影响

目的考察在丙二醇(propylene glycol,PG)-肉豆蔻酸异丙酯(isopropyl myristate,IPM)系统(简称PI系统)中经皮促透剂对来曲唑经皮透过性的影响。方法采用水平双室扩散池,以离体大鼠皮肤作为透过屏障进行体外透过实验。结果在不含经皮促透剂时,来曲唑的累积透过量随体系中PG浓度的增加而增大。在PI系统m(PG)∶m(IPM)=20∶100]中,N-甲基-2-吡咯烷酮、月桂氮卓酮、乳酸对来曲唑的透过具有显著的促进作用,司盘-80和二乙二醇单乙基醚具有轻微抑制作用,而油酸和吐温-80则有显著的抑制作用。结论在PI系统中经皮促透剂对来曲唑的经皮透过性具有不同的促透作用,为开发来曲唑的透皮给药贴剂提供参考数据。

Effects of enhancers on the skin permeation of letrozole in the PG -IPM system

Objective To assess the effect of penetration enhancers on the percutaneous permeability of letrozole in the propylene glycol and isopropyl myristate (PG-IPM, PI) system. Methods The modified Franz diffusion cells were adopted as the apparatus for skin permeation, excised rat abdominal skin as barrier. Results The accumulative permeation of letrozole increased with the increase of PG concentration in the systems containing no enhancers. In the PI m(PG)∶m(IPM)=20∶100] system, NMP, azone and lactic acid showed significant enhancing effect while span-80 and Transcutol^® P moderately decreased letrozole penetration. Oleic acid and tween-80 had significant inhibition activity on letrozole permeability in this system. Conclusions The effect of different penetration enhancers on the percutaneous permeability of letrozole in the PI system is different. The results obtained from this study will be helpful in the development of transdermal patch of letrozole.