Wiechers J W
Bioanalysis and Toxicology Group, University of Groningen, The Netherlands.
Pharm Weekbl Sci. 1989 Dec 15;11(6):185-98. doi: 10.1007/BF01959410.
There is currently a high level of interest in using the skin as a route for delivering drugs. The skin, however, provides an efficient barrier against percutaneous absorption of drugs. This barrier function can be ascribed to the macroscopical structure of the stratum corneum, which consists of alternating lipoidal and hydrophylic regions. For this reason, physico-chemical characteristics of the drug, such as partition coefficient and molecular weight, play an important role in determining the facility of percutaneous absorption. Another factor to consider in transdermal drug delivery, is the vehicle in which the drug is formulated as it acts on the release of drug from the formulation. Moreover, vehicles may also interact with human stratum corneum, thereby affecting its barrier function. Surfactants and penetration enhancers are well-known examples of the latter. Subsequently, dosing conditions, such as humidity, temperature and occlusion, also have their impact on the actual input (rate) of drug through human skin. Finally, all bits of information are combined to form a reasonably faithful picture of percutaneous absorption.
目前,人们对利用皮肤作为药物递送途径有着浓厚的兴趣。然而,皮肤对药物的经皮吸收提供了有效的屏障。这种屏障功能可归因于角质层的宏观结构,角质层由交替的脂质区域和亲水区域组成。因此,药物的物理化学特性,如分配系数和分子量,在决定经皮吸收的难易程度方面起着重要作用。透皮给药中另一个需要考虑的因素是药物制剂所用的载体,因为它会影响药物从制剂中的释放。此外,载体也可能与人体角质层相互作用,从而影响其屏障功能。表面活性剂和渗透促进剂就是后者的典型例子。随后,给药条件,如湿度、温度和封闭性,也会对药物通过人体皮肤的实际输入(速率)产生影响。最后,所有这些信息结合起来,形成了一幅关于经皮吸收的较为准确的图景。