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ZJUS-B
Journal of Zhejiang University-SCIENCE B (Biomedicine & Biotechnology)  2014, Vol. 15 Issue (11): 940-952    DOI: 10.1631/jzus.B1400158
Articles     
Essential oil from Zanthoxylum bungeanum Maxim. and its main components used as transdermal penetration enhancers: a comparative study
Yi Lan, Hui Li, Yan-yan Chen, Ye-wen Zhang, Na Liu, Qing Zhang, Qing Wu
School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China
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Abstract  Our previous studies had confirmed that the essential oil from Zanthoxylum bungeanum Maxim. (Z. bungeanum oil) could effectively enhance the percutaneous permeation of drug molecules as a natural transdermal penetration enhancer. The aim of the present study is to investigate and compare the skin penetration enhancement effect of Z. bungeanum oil and its main components on traditional Chinese medicine (TCM) active components. Toxicities of Z. bungeanum oil and three selected terpene compounds (terpinen-4-ol, 1,8-cineole, and limonene) in epidermal keratinocytes (HaCaT) and dermal fibroblast (CCC-ESF-1) cell lines were measured using an MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. Five model drugs in TCM external preparations, namely osthole (OT), tetramethylpyrazine (TMP), ferulic acid (FA), puerarin (PR), and geniposide (GP), which were selected based on their lipophilicity denoted by logKo/w, were tested using in vitro permeation studies in which vertical Franz diffusion cells and rat abdominal skin were employed. The secondary structure changes of skin stratum corneum (SC) and drug thermodynamic activities were investigated to understand their mechanisms of action using Fourier transform infrared (FTIR) spectroscopy and saturation solubility studies, respectively. It was found that Z. bungeanum oil showed lower toxicities in both HaCaT cells and CCC-ESF-1 cells compared with three terpene compounds used alone. The enhancement permeation capacities by all tested agents were in the following increasing order: terpinen-4-ol≈1,8-cineole<limonene<Z. bungeanum oil. The mechanisms of permeation enhancement suggested that these enhancers promoted the skin permeation of drugs mainly by affecting SC lipids. These results indicated that Z. bungeanum oil exhibited better performance in enhancing the skin permeation of active components in TCM preparations.

Key words： Zanthoxylum bungeanum Maxim.      Essential oil      Limonene      Fourier transform infrared (FTIR) spectroscopy      Penetration enhancer      HaCaT     
Received: 05 June 2014      Published: 04 November 2014
CLC:  R283  
  O65  
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Yi Lan
Hui Li
Yan-yan Chen
Ye-wen Zhang
Na Liu
Qing Zhang
Qing Wu
Cite this article:

Yi Lan, Hui Li, Yan-yan Chen, Ye-wen Zhang, Na Liu, Qing Zhang, Qing Wu. Essential oil from Zanthoxylum bungeanum Maxim. and its main components used as transdermal penetration enhancers: a comparative study. Journal of Zhejiang University-SCIENCE B (Biomedicine & Biotechnology), 2014, 15(11): 940-952.

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http://www.zjujournals.com/xueshu/zjus-b/10.1631/jzus.B1400158     OR     http://www.zjujournals.com/xueshu/zjus-b/Y2014/V15/I11/940

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