摘要
The aim of this present study is to investigate the effect of Zanthoxylum bungeanum oil （essential oil from Z. bungeanum Maxim.） on cytotoxicity and the transdermal permeation of 5-fluorouracil and indomethacin. The cy- totoxicity of Z. bungeanum oil on dermal fibroblasts and epidermal keratinocytes was studied using an MTT （3-（4,5-dimethylthiazol-2-yl）-2,5-diphenyltetrazolium bromide） assay. The rat skin was employed to determine the percutaneous penetration enhancement effect of Z. bungeanum oil on hydrophilic and lipophilic model drugs, i.e., 5-fluorouracil and indomethacin. The secondary structure changes of the rat stratum comeum （SC） were determined using attenuated total reflectance-Fourier transform infrared spectroscopy （ATR-FTIR）, and saturated solubilities and SC/vehicle partition coefficients of two model drugs with and without Z. bungeanum oil were also measured to un- derstand its related mechanisms of action. It was found that the half maximal inhibitory concentration （ICs0） values of Z. bungeanum oil were significantly lower in HaCaT and CCC-ESF-1 cell lines compared to the well-established and standard penetration enhancer Azone. The Z. bungeanum oil at various concentrations effectively facilitated the percutaneous penetration of two model drugs across the rat skin. In addition, the mechanisms of permeation en- hancement by Z. bungeanum oil could be explained with saturated solubility, SC/vehicle partition coefficient, and secondary structure changes of SC.
研究目的:研究花椒挥发油作为天然经皮促透剂的促透活性及其促透机制,同时评价其皮肤细胞毒性。创新要点:首次评价了花椒挥发油的皮肤细胞毒性、经皮促透活性及其作用机制。研究方法:利用表皮角质形成细胞(HaCaT)和真皮成纤维细胞(CCC-ESF-1)评价花椒挥发油的细胞毒性;采用亲水性及亲脂性模型药测定挥发油促透活性的基础上研究其促透作用机制。重要结论:花椒挥发油具有良好促透活性并具有较低皮肤细胞毒性。
基金
supported by the National Natural Science Foundation of China(No.81073059)
the Beijing Natural Science Foundation(No.7132127)
the Innovative Research Team in Beijing University of Chinese Medicine(No.2011-CXTD-13),China
