Transdermal drug delivery: Penetration enhancement techniques
Transdermal drug delivery: Penetration enhancement techniques
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DOI：
10.2174/1567201052772915
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发表时间：
2005-01-05
影响因子：
2.4
通讯作者：
Benson, Heather A. E.
中科院分区：
文献类型：
--
作者：
Benson, Heather A. E.
皮肤作为局部和全身作用的药物应用部位具有相当大的兴趣。然而，皮肤，特别是角质层，对药物渗透构成了强大的屏障，从而限制了局部和透皮生物利用度。已经开发了皮肤渗透增强技术以提高生物利用度并增加局部和经皮递送是可行选择的药物范围。本文综述了基于药物/载体优化的增强技术，如药物选择、前药和离子对、过饱和药物溶液、共晶系统、络合、脂质体、囊泡和颗粒。还讨论了通过水合作用、作用于角质层脂质和角蛋白的结构的化学增强剂、分配和溶解度效应来修饰角质层的增强。介绍了渗透促进剂和阻滞剂的作用机制及其临床应用潜力。
There is considerable interest in the skin as a site of drug application both for local and systemic effect. However, the skin, in particular the stratum corneum, poses a formidable barrier to drug penetration thereby limiting topical and transdermal bioavailability. Skin penetration enhancement techniques have been developed to improve bioavailability and increase the range of drugs for which topical and transdermal delivery is a viable option. This review describes enhancement techniques based on drug/vehicle optimisation such as drug selection, prodrugs and ion-pairs, supersaturated drug solutions, eutectic systems, complexation, liposomes, vesicles and particles. Enhancement via modification of the stratum corneum by hydration, chemical enhancers acting on the structure of the stratum corneum lipids and keratin, partitioning and solubility effects are also discussed. The mechanism of action of penetration enhancers and retarders and their potential for clinical application is described.