The majority of known peptides with high bioactivity (BAPs) such as antihypertensive, antidiabetic, antioxidant, hypocholesterolemic, anti-inflammatory and antimicrobial actions, are short-chain sequences of less than ten amino acids. These short-chain BAPs of varying natural and synthetic origin must be bioaccessible to be capable of being adsorbed systemically upon oral administration to show their full range of bioactivity. However, in general, in vitro and in vivo studies have shown that gastrointestinal digestion reduces BAPs bioactivity unless they are protected from degradation by encapsulation. This review gives a critical analysis of short-chain BAP encapsulation and performance with regard to the oral delivery route. In particular, it focuses on short-chain BAPs with antihypertensive and antidiabetic activity and encapsulation methods via nanoparticles and microparticles. Also addressed are the different wall materials used to form these particles and their associated payloads and release kinetics, along with the current challenges and a perspective of the future applications of these systems.

中文翻译：

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用于胃肠道输送的短链生物活性肽（BAP）的封装：综述

大多数已知的具有高生物活性（BAP）的肽，如抗高血压、抗糖尿病、抗氧化、降胆固醇、抗炎和抗菌作用，都是少于十个氨基酸的短链序列。这些不同天然和合成来源的短链 BAP 必须具有生物可访问性，能够在口服给药时被全身吸收，以显示其全方位的生物活性。然而，一般而言，体外和体内研究表明，胃肠道消化会降低 BAP 的生物活性，除非通过封装保护它们免遭降解。本综述对短链 BAP 封装和口服给药途径的性能进行了批判性分析。它特别关注具有抗高血压和抗糖尿病活性的短链 BAP 以及通过纳米颗粒和微米颗粒的封装方法。还讨论了用于形成这些颗粒的不同壁材料及其相关的有效负载和释放动力学，以及这些系统当前的挑战和未来应用的前景。