热性中药挥发油透皮促渗不同成分的规律性研究

Study on the Regularity of Essential Oils from Traditional Chinese Medicine with Hot Property in Enhancing Skin Permeability of Different Components

  • 摘要:
    目的 阐明热性中药挥发油透皮促渗不同成分的规律性。
    方法 以五种热性中药挥发油(高良姜油、干姜油、肉桂油、胡椒油、吴茱萸油)为研究对象,以常用化学促渗剂(Penetration enhancer, PE)氮酮为对照,首先考察皮肤安全性,然后在建立分析方法的基础上,采用改良Franz扩散池法进行体外透皮实验以考察热性中药挥发油透皮促渗9种中药成分的效果。
    结果 5种热性中药挥发油皮肤细胞毒性IC50值是氮酮的3.63~8.15倍。HPLC方法专属性良好,各成分均有良好的线性关系、精密度、重复性、稳定性和准确性。热性中药挥发油的透皮促渗效果与所促渗成分的油水分配系数相关,对于logP在2.6~3.5范围内的亲脂性成分如白藜芦醇、延胡索乙素、槲皮素等促渗效果较好。
    结论 应根据促渗成分的油水分配系数合理选用热性中药挥发油透皮促渗剂。

     

    Abstract:
    OBJECTIVE To study regularity of different components whose skin permeability is enhanced by essential oils (EOs) from traditional Chinese medicine (TCM) with hot property.
    METHODS Five EOs from TCM with hot property, namely Galangal oil, Dried Ginger oil, Cinnamon oil, Pepper oil, and Evodia oil were prepared and used in further studies. The in vitro skin cytotoxicity of these EOs and chemical penetration enhancer (PE) Azone were compared. HPLC method was established to determine 9 TCM components that are usually used in permeation studies. And the in vitro permeation experiments were carried out using the modified Franz diffusion cell method to evaluate the penetration enhancement effects of five EOs.
    RESULTS The cytotoxicity test revealed the IC50 value of EOs was 3.63-8.15 times of that of Azone, the classical chemical PE. HPLC method showed perfect specificity and 9 TCM components performed well in linear relationship, precision, repeatability, stability, and average recovery rate. The results of multiple linear regression showed a significant association between the penetration enhancement effects of EOs from TCM with hot property and logP values of the TCM components. EOs from TCM with hot property showed satisfactory penetration enhancement effects for hydrophobic components with logP values in the range of 2.6-3.5, e.g. resveratrol, tetrahydropalmatine and quercetin.
    CONCLUSION EOs from TCM with hot property should be reasonably selected as PE according to the oil-water partition coefficient of the ingredients.

     

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