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
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摘要: 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。Abstract: 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.
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