Key Laboratory of Sensing Technology and Biomedical Instrument of Guangdong, Province, School of Biomedical Engineering, Sun Yat-sen University, Guangzhou, Guangdong 510006, PR China.
Biomater Sci. 2020 Nov 7;8(21):5804-5823. doi: 10.1039/d0bm01151g. Epub 2020 Oct 5.
In recent years, peptide/protein drugs have attracted considerable attention owing to their superior targeting and therapeutic effect and fewer side effects compared with chemical drugs. Oral administration modality with enhanced patient compliance is increasingly being recognized as an ideal route for peptide/protein delivery. However, the limited permeation efficiency and low oral bioavailability of peptide/protein drugs significantly hinder therapeutic advances. To address these problems, various nano and microscale delivery platforms have been developed, which offer significant advantages in oral peptide/protein delivery. In this review, we briefly introduce the transport mechanisms of oral peptide/protein delivery and the primary barriers to this delivery process. We also highlight the recent advances in various nano and microscale delivery platforms designed for oral peptide/protein delivery. We then summarize the existing strategies used in these delivery platforms to improve the oral bioavailability and permeation efficiency of peptide/protein therapeutics. Finally, we discuss the major challenges faced when nano and microscale systems are used for oral peptide/protein delivery. This review is expected to provide critical insight into the design and development of oral peptide/protein delivery systems with significant therapeutic advances.
近年来，与化学药物相比，肽/蛋白质药物因其具有更好的靶向性和治疗效果以及更少的副作用而引起了广泛关注。增强患者依从性的口服给药方式越来越被认为是肽/蛋白质递药的理想途径。然而，肽/蛋白质药物的有限渗透效率和低口服生物利用度极大地阻碍了治疗进展。为了解决这些问题，已经开发了各种纳米和微尺度的给药平台，它们在口服肽/蛋白质递药方面具有显著的优势。在本综述中，我们简要介绍了口服肽/蛋白质递药的转运机制以及该递药过程中的主要障碍。我们还重点介绍了为口服肽/蛋白质递药设计的各种纳米和微尺度给药平台的最新进展。然后，我们总结了这些递药平台中用于提高肽/蛋白质治疗剂口服生物利用度和渗透效率的现有策略。最后，我们讨论了纳米和微尺度系统用于口服肽/蛋白质递药时面临的主要挑战。本综述有望为具有显著治疗进展的口服肽/蛋白质递药系统的设计和开发提供重要的见解。
