Karande Pankaj, Mitragotri Samir
Department of Chemical and Biological Engineering, Rensselaer Polytechnic Institute, Troy, NY 12180, USA.
Biochim Biophys Acta. 2009 Nov;1788(11):2362-73. doi: 10.1016/j.bbamem.2009.08.015. Epub 2009 Sep 3.
Transdermal drug delivery is an attractive alternative to conventional techniques for administration of systemic therapeutics. One challenge in designing transdermal drug delivery systems is to overcome the natural transport barrier of the skin. Chemicals offer tremendous potential in overcoming the skin barrier to enhance transport of drug molecules. Individual chemicals are however limited in their efficacy in disrupting the skin barrier at low concentrations and usually cause skin irritation at high concentrations. Multicomponent mixtures of chemicals, however, have been shown to provide high skin permeabilization potency as compared to individual chemicals without necessarily causing irritation. Here we review systems employing synergistic mixtures of chemicals that offer superior skin permeation enhancement. These synergistic systems include solvent mixtures, microemulsions, eutectic mixtures, complex self-assembled vesicles and inclusion complexes. Methods for design and discovery of such synergistic systems are also discussed.
经皮给药是全身治疗药物传统给药技术的一种有吸引力的替代方法。设计经皮给药系统的一个挑战是克服皮肤的天然转运屏障。化学物质在克服皮肤屏障以增强药物分子转运方面具有巨大潜力。然而，单个化学物质在低浓度下破坏皮肤屏障的功效有限，并且在高浓度下通常会引起皮肤刺激。然而，与单个化学物质相比，化学物质的多组分混合物已被证明能提供高皮肤通透效力，且不一定会引起刺激。在此，我们综述了采用化学物质协同混合物以实现卓越皮肤渗透增强效果的系统。这些协同系统包括溶剂混合物、微乳液、低共熔混合物、复杂自组装囊泡和包合物。还讨论了此类协同系统的设计和发现方法。
