主 办:北 京 中 医 药 大 学
ISSN 1006-2157 CN 11-3574/R

JOURNAL OF BEIJIGN UNIVERSITY OF TRADITIONAL CHINE ›› 2016, Vol. 39 ›› Issue (2): 155-161.doi: 10.3969/j.issn.1006-2157.2016.02.014

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Percutaneous penetration enhancement effects of azone on TCM active ingredients with different lipophilicity*

WANG Jingyan1, LAN Yi1,2, RU Qingguo1, WANG Yifei1, LIU Yan1, YU Jingxin1, WU Qing1#   

  1. 1 School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102;
    2 Ovation Health Science and Technology Co.Ltd, ENN Group, Hebei
  • Received:2015-03-10 Online:2016-02-28 Published:2016-02-28

Abstract: Objective To investigate the effects of azone on transdermal absorption of TCM active ingredients with different lipophilicity, and further explore its percutaneous penetration enhancement effects on the complex TCM active ingredients. Methods Five model drugs, namely osthole, tetramethylpyrazine,ferulic acid, puerarin and geniposide, were selected based on their lipophilicity determined by logKo/w, and then tested using in vitro permeation studies in which Franz diffusion cellsand rat skin were employed.Meanwhile, the association between the logKo/w values of model drugs and enhancement ratio(ER) was established. Results Different concentrations of azone could significantly promote the transdermal absorption of all model drugs. The ER value gradually increased with the increase of the azone concentration withina certain concentration range. It, however, started to decrease when exceedinga certain concentration level. The penetration enhancement ratio was roughly in parabolic curve relation with the drug lipophilicity after treatment with azone, and azone could achieve the optimal permeation effect for moderate hydrophilic drugs (an estimated logKo/w value of -0.5). Conclusion azone could significantly promote the transdermal absorption of TCM components with different lipophilicity, and its penetration enhancement ratio was in parabolic curve relation with the drug lipophilicity.

Key words: azone, TCM active ingredients with different lipophilicity, penetration enhancer, transdermal absorption

CLC Number: 

  • R284