Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Mercer University, 3001 Mercer University Drive, Atlanta, Georgia 30341, USA.
AAPS PharmSciTech. 2011 Mar;12(1):431-41. doi: 10.1208/s12249-011-9601-6. Epub 2011 Mar 3.
Transdermal delivery of peptides and proteins avoids the disadvantages associated with the invasive parenteral route of administration and other alternative routes such as the pulmonary and nasal routes. Since proteins have a large size and are hydrophilic in nature, they cannot permeate passively across the skin due to the stratum corneum which allows the transport of only small lipophilic drug molecules. Enhancement techniques such as chemical enhancers, iontophoresis, microneedles, electroporation, sonophoresis, thermal ablation, laser ablation, radiofrequency ablation and noninvasive jet injectors aid in the delivery of proteins by overcoming the skin barrier in different ways. In this review, these enhancement techniques that can enable the transdermal delivery of proteins are discussed, including a discussion of mechanisms, sterility requirements, and commercial development of products. Combination of enhancement techniques may result in a synergistic effect allowing increased protein delivery and these are also discussed.
经皮传递肽和蛋白质可避免与侵入性的肠外给药途径和其他替代途径（如肺部和鼻腔途径）相关的缺点。由于蛋白质体积较大且具有亲水性，因此由于角质层的存在，它们不能被动地透过皮肤扩散，角质层仅允许小的亲脂性药物分子通过。化学增强剂、离子电渗、微针、电穿孔、声流、热消融、激光消融、射频消融和非侵入性射流注射器等增强技术通过以不同方式克服皮肤屏障来帮助蛋白质的传递。在这篇综述中，讨论了这些可以实现蛋白质经皮传递的增强技术，包括对机制、无菌要求和产品的商业开发的讨论。增强技术的组合可能会产生协同作用，从而增加蛋白质的传递，这也将进行讨论。
