基于药性特征的中药挥发油透皮促渗作用规律性认识的思路与方法

应用透皮促渗剂(penetration enhancers,PE)是解决外用制剂吸收难题的最常用方法之一。中药挥发油是一大类性质优良的PE,品种总数达到300余种,而目前有作为PE报道的中药挥发油仅为34种,近90%的中药挥发油从未作为PE应用,研究开发潜力巨大。但是目前其研究主要是遵循化学促渗剂的研究思路,通过透皮促渗效果和药效学评价来进行筛选,效率不高。中药挥发油是中药辛味的主要物质基础,药性理论有"辛能开腠理"的认识,文献研究发现中药挥发油透皮促渗效果与药性特征显著关联,在此基础上,提出了"中药挥发油透皮促渗作用存在药性特征规律"的观点,并提出了基于系统研究和数据挖掘阐明药性特征规律,从不同类型中药挥发油中选择和发现高效低毒的透皮促渗剂的研究思路;提出了应用脂质体人工皮肤膜技术结合评价指标优选,实现高通量评价中药挥发油PE促渗效果的研究方法与技术,为中药挥发油PE的研究、传统中药药性理论与现代PE研究的结合提供了新的策略与方法。此外,还提出了微乳型制剂研究可能是中药挥发油PE研究的未来发展方向。

Idea and method of regularity knowledge of Chinese materia medica on essential oils as potential penetration enhancers based on drug property characteristics

Penetration enhancers (PE) were usually applied as the optimum strategy to improve the percutaneous absorption of active components from pharmaceutical preparations. Essential oils (EOs) were a kind of PE with satisfactory characteristics. Only 34 of among more than 300 EOs are reported to be used as PE. That is to say, about 90% EOs have not been applied until now and EOs possess great potential to act as PE. However, the research of EOs from Chinese materia medica (CMM) mainly followed the strategy of chemical PE. A large amount of studies were carried out to evaluate the transdermal penetration enhancing efficacy and pharmacological activity, resulting in the limited efficiency. EOs of CMM were also the key material basis of CMM pungent flavor. In the theory of traditional Chinese medicines (TCM), it was accepted that the pungent flavor could open the striae and interstice. The results of literature investigation revealed that the penetration enhancing efficacy of EOs directly related with drug property characteristics of CMM. Therefore, in the present paper, it was proposed that a rule existed between the penetration enhancing efficacy of EOs and drug property characteristics of CMM. A series of studies were then designed to reveal the rule with the aid of data analysis. The resultant rule will help to find the effective PE from various EOs. Moreover, to facilitate the high-throughput screening of EOs, liposomal artificial skin membrane was prepared and applied to the evaluation of in vitro penetration enhancing efficacy of EOs with optimization of the evaluation parameters. Finally, the results of the study will provide a novel strategy for the research of EOs as PE and the research of the application of TCM theory to the modern pharmaceutical study. In addition, the application of microemulsion technique will be the future trends of EOs as PE to solve the stability problems.