冬青油促进蛇床子素和桅子苷透皮吸收的研究

Effect of wintergreen oil on in vitro transdermal permeation of osthole and geniposide

该文拟研究冬青油的体外经皮促渗效果及其作用机制。选择蛇床子素和桅子苷作为亲脂性和亲水性模型药物,利用体外透皮试验测定冬青油的经皮促透效果;采用傅利叶变换红外光谱技术研究冬青油对大鼠皮肤角质层分子结构的影响,并利用扫描电镜直观观察冬青油对大鼠皮肤表皮的影响,探讨其经皮促透机制。结果表明,当冬青油达到一定应用浓度后对蛇床子素和桅子苷均具良好经皮促透效果,但对蛇床子素的促透效果更佳,接近于常用经典促透剂月桂氮酮;红外光谱和扫描电镜研究显示,冬青油主要作用于皮肤角质层脂质,降低角质层致密排列,从而降低皮肤屏障作用。由此可知,冬青油作为促透剂可有效增加亲脂性和亲水性药物的透皮吸收,且对亲脂性药物促透效果更佳,这与其作用于皮肤角质层脂质而改变皮肤表层致密结构有关。

The aim of this study was to investigate the transdermal penetration enhancement effect of wintergreen oil and its action mechanisms.The in vitro transdermal tests were carried out to study the transdermal penetration enhancement effect of wintergreen oil by using osthole and geniposide as the lipophilic and hydriphilic model drugs.Fourier-transform infrared spectroscopy was used to investigate the effect of wintergreen oil on the molecular structure of rat stratum corneum,and the scanning electron microscope was employed to observe the change of rat skin surface after treatment by the oil.The wintergreen oil at proper concentrations could effectively promote the transdermal permeation of osthole and geniposide,and exhibited better penetration-enhancing activity for the lipophilic osthole,close to the commonly used classical penetration enhancer azone.The infrared spectroscopy study and scanning electron microscope showed that wintergreen oil mainly acted on the stratum corneum lipids,reduced dense stratum corneum,and reduced the skin barrier function.Thus,the wintergreen oil could effectively facilitate the transdermal absorption of the lipophilic and hydrophilic drugs,resulting from the lowed skin barrier function.