title: Cytotoxicity and enhancement activity of essential oil from Zanthoxylum bungeanum Maxim. as a natural transdermal penetration enhancer.
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.
authors: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China; Center of Science Experiment, Beijing University of Chinese Medicine, Beijing 100029, China.
authors: Yi
authors: Y
authors: Lan
authors: Qing
authors: Q
authors: Wu
authors: Ying-qiu
authors: YQ
authors: Mao
authors: Qiong
authors: Q
authors: Wang
authors: Jing
authors: J
authors: An
authors: Yan-yan
authors: YY
authors: Chen
authors: Wen-ping
authors: WP
authors: Wang
authors: Bo-chen
authors: BC
authors: Zhao
authors: Na
authors: N
authors: Liu
authors: Ye-wen
authors: YW
authors: Zhang
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D002460:Cell Line; D045744:Cell Line, Tumor; D005347:Fibroblasts / Q000187:drug effects*; D005472:Fluorouracil / Q000008:administration & dosage; D006801:Humans; D007213:Indomethacin / Q000008:administration & dosage; D020128:Inhibitory Concentration 50; D015603:Keratinocytes / Q000187:drug effects*; D008297:Male; D009822:Oils, Volatile / Q000737:chemistry*; D010938:Plant Oils / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000187:drug effects* / Q000378:metabolism; D012869:Skin Absorption; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013778:Tetrazolium Salts; D013844:Thiazoles; D032106:Zanthoxylum / Q000737:chemistry*
chemical_list: D009822:Oils, Volatile; D010938:Plant Oils; D013778:Tetrazolium Salts; D013844:Thiazoles; C022616:thiazolyl blue; D005472:Fluorouracil; D007213:Indomethacin