Basics and recent advances in peptide and protein drug delivery.
Basics and recent advances in peptide and protein drug delivery.
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DOI：
10.4155/tde.13.104
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发表时间：
2013-11
影响因子：
4.2
通讯作者：
Lim CS
中科院分区：
文献类型：
--
作者：
Bruno BJ;Miller GD;Lim CS
虽然肽和蛋白质治疗市场在过去几十年中有了显着发展，但递送限制了它们的使用。尽管口服递送是优选的，但由于在胃肠道中的降解和有限吸收，目前大多数是静脉内或皮下递送。因此，正在研究吸收促进剂、酶抑制剂、载体系统和稳定性增强剂以促进口服肽递送。此外，经皮肽递送避免了胃肠道的问题，但也面临吸收限制。由于蛋白酶、调理作用和凝集，游离肽在没有修饰的情况下不是系统稳定的。这篇综述讨论了口服和经皮肽药物递送，重点是吸收和稳定性问题的障碍和解决方案。还讨论了增加全身稳定性和位点特异性递送的方法。
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.