Bruno Benjamin J, Miller Geoffrey D, Lim Carol S
Department of Pharmaceutics & Pharmaceutical Chemistry, College of Pharmacy, University of Utah. 30 South 2000 East, Room 301, Salt Lake City, UT 84112, USA.
Ther Deliv. 2013 Nov;4(11):1443-67. doi: 10.4155/tde.13.104.
While the peptide and protein therapeutic market has developed significantly in the past decades, delivery has limited their use. Although oral delivery is preferred, most are currently delivered intravenously or subcutaneously due to degradation and limited absorption in the gastrointestinal tract. Therefore, absorption enhancers, enzyme inhibitors, carrier systems and stability enhancers are being studied to facilitate oral peptide delivery. Additionally, transdermal peptide delivery avoids the issues of the gastrointestinal tract, but also faces absorption limitations. Due to proteases, opsonization and agglutination, free peptides are not systemically stable without modifications. This review discusses oral and transdermal peptide drug delivery, focusing on barriers and solutions to absorption and stability issues. Methods to increase systemic stability and site-specific delivery are also discussed.
在过去几十年中，肽和蛋白质治疗市场取得了显著发展，但给药方式限制了它们的应用。尽管口服给药是首选，但由于在胃肠道中会降解且吸收有限，目前大多数肽和蛋白质药物是通过静脉注射或皮下注射给药。因此，人们正在研究吸收增强剂、酶抑制剂、载体系统和稳定性增强剂，以促进口服肽给药。此外，经皮肽给药避免了胃肠道问题，但也面临吸收限制。由于蛋白酶、调理作用和凝集作用，未经修饰的游离肽在体内并不稳定。本文综述了口服和经皮肽药物递送，重点讨论了吸收和稳定性问题的障碍及解决方案。还讨论了提高全身稳定性和定点递送的方法。
