透皮给药研究的新进展

New progress in transdermal drug delivery

透皮给药安全可控,是无创给药的新途径,有着广阔的市场前景。现有的透皮药物限于小分子和低浓度,角质层屏障使大多数药物难以通过或难以达到有效浓度和有效速率。透皮给药的关键在于促进药物渗透,使药物透皮吸收进毛细血管。促渗手段有:使用化学促渗剂;对药物进行化学修饰制成前体药物;使用物理方法;将药物载入载体。这些方法的原理大致分为三种:改变角质层结构;外力驱动药物;将药物进行修饰或包裹。简要地介绍了增强药物透皮的物理方法和载体方法研究的新进展。

Transdermal drug delivery systems have been widely accepted for administration because of increased patient acceptability, avoidance of gastrointestinal disturbances and bypassing of hepatic first-pass metabolism. However, transdermal delivery is severely limited by the inability of the large majority of drugs to cross skin at therapeutic rates. The transdermal paths are stratum corneum and attachments of skin. The area of attachments is very small so the compact stratum corneum is the main barrier especially for macromolecules. Many approaches have been used to overcome the barrier including chemical enhancement, physical enhancement and carrier enhancement. The current researches focused on modifying the structure of the stratum corneum, driving drugs with force and loading drugs into carriers. Besides, the combination of several approaches reinforces the enhancement effect. Several transdermal drug deliveries have entered the market successfully. In the future, drugs of wider range will come into use. This paper introduces the new progress of physical method and carrier method for enhancing delivery.