目的 研究细辛Asari Radix et Rhizoma挥发油促进芥子碱经皮渗透及其机制。方法 首先采用经皮水分丢失仪测定细辛挥发油作用后皮肤经皮水分丢失的变化，以此来确定细辛挥发油作用皮肤后是否降低皮肤屏障功能。然后以SD大鼠背部皮肤作为渗透屏障，利用扩散池法研究细辛挥发油对芥子碱的体外经皮累积渗透量及皮肤滞留量的影响；并通过SD大鼠在体经皮给药测定给药24 h后皮肤中芥子碱透过量，进一步验证细辛挥发油对芥子碱的促渗作用。随后，利用全反射傅里叶红外变换光谱（ATR-FTIR）和差示扫描量热法（DSC）表征细辛挥发油作用后大鼠皮肤角质层中脂质和蛋白变化，观察细辛挥发油对大鼠皮肤角质层脂质和蛋白的影响。结果 皮肤经皮水分丢失率（TEWL）测定结果表明，细辛挥发油作用于大鼠皮肤后，TEWL值升高，皮肤屏障功能降低。离体透皮实验结果表明含细辛挥发油组的芥子碱的经皮累积渗透量及皮肤滞留量都明显高于不含细辛挥发油组；在体透皮实验进一步验证了细辛挥发油促进芥子碱在皮肤的滞留。ATR-FTIR和DSC结果表明，与细辛挥发油未作用组相比，细辛挥发油作用后皮肤角质层中的脂质和角蛋白构象发生紊乱，皮肤的渗透性增加。结论 细辛挥发油可促进芥子碱的经皮渗透，其促透机制与细辛挥发油紊乱皮肤角质脂质和蛋白的流动性相关。

Objective To study the enhancing effect of essential oil from asarum (EOA) on percutaneous delivery of sinapine and its mechanism. Methods Transepidermal water loss (TEWL) was determined with Vapo Meter to evaluate the decrease of skin barrier by asarum essential oil. In vitro permeation of sinapine through rat skin was performed in the presence or absence of EOA, and the permeated cumulative amount and retention of sinapine were compared. In vivo percutaneous test was further performed to estimate the improvement of EOA on percutaneous delivery of sinapine. Attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR) and differential scanning calorimeter (DSC) were used to evaluate the changes of lipid and protein in stratum corneum. Results TEWL value increased after the treatment of EOA, which indicated the decrease of skin barrier. The permeated cumulative amount and retention of sinapine in the presence of EOA were higher than those in the absence of EOA, and in vivo percutaneous test further confirmed this issue. After EOA treatment, the lipid and protein disorder could be observed from ATR-FTIR and DSC map, which indicated the increasing of skin permeability. Conclusion EOA can enhance the percutaneous delivery of sinapine through improving the disorder of lipid and protein of stratum corneum.

国家自然科学基金资助项目（81073066，81473358）