肽和蛋白质药物传递的基础和最新进展

S.D. Mankar, Bhagyashri S. Jadhav, Awantika N. Kale
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引用次数: 11

摘要

虽然肽和蛋白质治疗市场在过去几十年中有了显著的发展,但递送限制了它们的使用。尽管口服给药是首选,但由于降解和胃肠道吸收有限,目前大多数是静脉或皮下给药,吸收促进剂、酶抑制剂、载体系统和稳定性增强剂正在研究中,以使口服肽递送更容易。同样,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、调理和凝集作用,游离肽在没有修饰的情况下不是系统稳定的。本文综述了口服和透皮多肽给药,重点讨论了吸收和稳定性问题的障碍和解决方案。还讨论了增加系统稳定性和特定部位递送的方法。
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Basics and Recent Advances in Peptide and Protein Drug Delivery
While the peptide and protein therapeutic market has developed significantly in the past decades, delivery has limited their use. Despite the fact oral delivery is preferred, most are currently delivered intravenously or subcutaneously due to degradation and limited absorption in the gastrointestinal tract, absorption enhancers, enzyme inhibitors, carrier systems and stability enhancers are being studied to make easier oral peptide delivery. As well, transdermal peptide delivery avoids the issues of the gastrointestinal tract, but also faces absorption limitations. Due to proteases, opsonisation 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.
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