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Cytotoxicity and enhancement activity of essential oil from Zanthoxylum bungeanum Maxim. as a natural transdermal penetration enhancer
摘    要:

收稿时间:2013 Aug 28

Cytotoxicity and enhancement activity of essential oil from Zanthoxylum bungeanum Maxim. as a natural transdermal penetration enhancer
Authors:Yi Lan  Qing Wu  Ying-qiu Mao  Qiong Wang  Jing An  Yan-yan Chen  Wen-ping Wang  Bo-chen Zhao  Na Liu  Ye-wen Zhang
Institution:1. School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, 100102, China
2. Center of Science Experiment, Beijing University of Chinese Medicine, Beijing, 100029, China
Abstract: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 cytotoxicity 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 corneum (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 understand its related mechanisms of action. It was found that the half maximal inhibitory concentration (IC50) 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 enhancement by Z. bungeanum oil could be explained with saturated solubility, SC/vehicle partition coefficient, and secondary structure changes of SC.
Keywords:Zanthoxylum bungeanum Maxim    Essential oil  Transdermal delivery  Penetration enhancer  HaCaT  Attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR)
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