Zhao Xin-Yu, Wang Jing-Yan, Deng Li-Li, Liu Yu-Juan, Guo Zi-You, Wu Qing
School of Chinese Materia Medica, Beijing University of Chinese Medicine Beijing 102488, China.
Zhongguo Zhong Yao Za Zhi. 2021 Oct;46(20):5284-5290. doi: 10.19540/j.cnki.cjcmm.20210129.303.
This study aimed to investigate the enhancing effect of muscone on the transdermal penetration of traditional Chinese medicine ingredients and explore its possible mechanism of action. The Franz diffusion cells were employed to investigate the effect of muscone on the transdermal permeation of a series of model drugs with a wide range of log P values. The solubilities at saturation and the stratum corneum(SC)/vehicle partition coefficients of model drugs were measured to evaluate the effect of muscone on drug thermodynamic activities and partition of drugs into SC. Attenuated total reflectance-Fourier transform infrared spectroscopy(ATR-FTIR) was employed to explore the effect of muscone on the molecular structure of SC. The results showed that muscone significantly promoted the transdermal penetration of hydrophilic and lipophilic drugs, and the enhancement ratio(ER) increased with the decrease in the log P. Muscone could interact with the SC lipids to increase the disorder and fluidity of lipid bilayer packing, which improved skin permeability and promoted transdermal absorption of drugs. This study provides a scientific basis for the application of muscone in traditional Chinese medicine topical preparations.
本研究旨在考察麝香酮对中药成分透皮渗透的增强作用，并探讨其可能的作用机制。采用Franz扩散池考察麝香酮对一系列具有广泛log P值的模型药物透皮渗透的影响。测定模型药物的饱和溶解度和角质层（SC）/载体分配系数，以评估麝香酮对药物热力学活性及药物在SC中分配的影响。采用衰减全反射-傅里叶变换红外光谱（ATR-FTIR）研究麝香酮对SC分子结构的影响。结果表明，麝香酮显著促进亲水性和疏水性药物的透皮渗透，增强率（ER）随log P值的降低而增加。麝香酮可与SC脂质相互作用，增加脂质双层堆积的无序性和流动性，从而改善皮肤通透性，促进药物透皮吸收。本研究为麝香酮在中药外用制剂中的应用提供了科学依据。
