几种挥发油对黄藤素透皮给药的促渗作用研究

Studies on the transdermal delivery of palmatine by several volatile oils as penetration enhancers

为给黄藤素透皮给药选择合适的挥发油促渗剂,以高效液相色谱法测定黄藤素的含量,采用立式扩散池法研究桉叶油、艾叶油、当归油、连翘油对黄藤素透皮给药的影响;实验结束后,用DSC扫描观察皮肤的特征峰变化。结果表明,5 h时,艾叶油组药物的累积透过量分别是被动扩散组、桉叶油组、当归油组、连翘油组的1.82,1.16,1.48,1.63倍,药物的累积渗透量随着艾叶油浓度的增加而增加,艾叶油浓度1.5%时,其促渗能力最强。DSC图谱表明,不同挥发油对皮肤的特征峰具有不同的影响,促渗能力较好的挥发油使皮肤的特征峰消失;当艾叶油的浓度由0.5%增加到1.5%,DSC图谱发生相应变化,浓度为1.5%和2.0%时具有相似的图谱,而浓度为2.5%时的DSC图谱与0.5%的图谱相似。艾叶油能够显著促进黄藤素的透皮给药,且最佳的浓度为1.5%,其机理可能是通过扰乱或破坏皮肤角质层的有序结构来增强皮肤对药物的渗透性,因此,艾叶油可作为黄藤素透皮给药的理想促渗剂而具有广泛的应用前景。

Choosing the best potential penetration enhancer（ PE） for the transdermal PA delivery. The amount of PA was determined by HPLC system. The vertical diffusion cells method was used to investigate the effects of volatile oils on the transdermal delivery of PA,the skin samples were also scanned by DSC at the end of the experiment. Result showed that,at 5. 0 h,the accumulated permeation amount of PA for the Artemisia oil group was 1. 82,1. 16,1. 48,1. 63 times. When the concentration of Artemisia oil reached 1. 5%,the accumulated permeation amount of PA was highest compared with other concentrations and passive diffusion groups. The results showed that the 1. 5% Artemisia oil is very suitable for the transdermal delivery of PA. DSC images showed that different volatile oils had different effects on the characteristic peaks of skin. When the skin treated by Artemisia oil,the characteristic peaks of skin diminished or disappeared,and appeared one new peak at about 80 ℃. These results suggested that Artemisia oil with the concentration of 1. 5% is more effective at enhancing permeation of PA through the skin,the mechanism may be that the dense and ordered structure of stratum corneum were disrupted and destroyed by Artemisia oil for the enhanced skin permeability.