挥发油含氧单萜成分的透皮吸收促进作用与皮肤细胞毒性比较研究

Comparative Study on Transdermal Penetration Enhancement and Cytotoxicity of Nine Oxygen-Containing Monoterpenes from Essential Oils

目的比较中药挥发油含氧单萜成分的透皮吸收促进作用与皮肤细胞毒性。方法以中药挥发油中常见的9种含氧单萜(1,8-桉叶素、4-萜品醇、樟脑、薄荷脑、α-松油醇、香芹酮、芳樟醇、香叶醇和柠檬醛)为研究对象,比较其对布洛芬的透皮吸收促进效果和对人角质形成细胞HaCaT的细胞毒性。结果 9种含氧单萜成分均能显著促进布洛芬的透皮吸收,且皮肤细胞毒性远低于经典的化学合成促渗剂氮酮,其中1,8-桉叶素的效果最好。环状含氧单萜(1,8-桉叶素、4-萜品醇、樟脑、薄荷脑、α-松油醇、香芹酮)的透皮吸收促进效果优于链状含氧单萜(芳樟醇、香叶醇、柠檬醛),皮肤细胞毒性没有显著差异。结论环状含氧单萜更适合作为透皮吸收促进剂进行开发。

OBJECTIVE To compare transdermal penetration enhancement and cytotoxicity of nine oxygen-containing monoterpenes from essential oils. METHODS The nine most common oxygen containing monoterpenes from herbal essential oils, which have penetration enhancement reports were selected. They are 1,8-cineole, 4-terpineol, camphor, menthol, α-terpineol, carvone, linalool, geraniol and citral. Its effect of permeation enhancement on ibuprofen and cytotoxicity on HaCaT cells were compared. RESULTS The nine oxygen containing monoterpenes all promoted the transdermal absorption of ibuprofen evidently, and the cytotoxicity were much lower than that of the classical chemical penetration enhancer azone. 1,8-cineole has the best effect. It was found that the cyclic oxygen containing monoterpenes（1,8-cineole, 4-terpineol, camphor, menthol, α-terpineol, carvone）have better penetration enhancement effect than that of the chain oxygen containing monoterpenes（linalool, geraniol, citral）. There was no significant difference between the cytotoxicity of cyclic and chain oxygen containing monoterpenes. CONCLUSION Cyclic oxygen-containing monoterpenes are more suitable for the development of penetration enhancers.