School of Food Science and Engineering, South China University of Technology/Guangdong Province Key Laboratory for Green Processing of Natural Products and Product Safety, Guangzhou, China.
Sericultural & Agri-Food Research Institute, Guangdong Academy of Agricultural Sciences/Key Laboratory of Functional Foods, Ministry of Agriculture and Rural Affairs/Guangdong Key Laboratory of Agricultural Products Processing, Guangzhou, China.
Crit Rev Food Sci Nutr. 2022;62(23):6341-6358. doi: 10.1080/10408398.2021.1900774. Epub 2021 Mar 22.
Lactoferrin (Lf), a bioactive protein initially found in many biological secretions including milk, is regarded as the nutritional supplement or therapeutic ligand due to its multiple functions. Research on its mode of action reveals that intact Lf or its active peptide (i.e., lactoferricin) shows an important multifunctional performance. Oral delivery is considered as the most convenient administration route for this bioactive protein. Unfortunately, Lf is sensitive to the gastrointestinal (GI) physicochemical stresses and lactoferricin is undetectable in GI digesta. This review introduces the functionality of Lf at the molecular level and its degradation behavior in GI tract is discussed in detail. Subsequently, the absorption and transport of Lf from intestine into the blood circulation, which is pivotal to its health promoting effects in various tissues, and some assisting labeling methods are discussed. Stabilization technologies aiming at preserving the structural integrity and functional properties of orally administrated Lf are summarized and compared. Altogether, this work comprehensively reviews the structure-function relationship of Lf, its oral fate and the development of stabilization technologies for the enhancement of the oral bioavailability of Lf. The existing limitations and scope for future research are also discussed.
乳铁蛋白（Lf）最初在包括牛奶在内的许多生物分泌物中被发现，是一种具有多种功能的生物活性蛋白，被认为是营养补充剂或治疗配体。对其作用模式的研究表明，完整的 Lf 或其活性肽（即乳铁蛋白肽）表现出重要的多功能性能。口服给药被认为是这种生物活性蛋白最方便的给药途径。不幸的是，Lf 对胃肠道（GI）的理化应激很敏感，而且 GI 消化液中检测不到乳铁蛋白肽。本综述介绍了 Lf 在分子水平上的功能及其在胃肠道中的降解行为，并进行了详细讨论。随后，讨论了 Lf 从肠道吸收并进入血液循环的情况，这对于其在各种组织中的促进健康作用至关重要，并讨论了一些辅助标记方法。总结并比较了旨在保持口服给予的 Lf 的结构完整性和功能特性的稳定化技术。总之，本工作全面综述了 Lf 的结构-功能关系、其口服命运以及稳定化技术的发展，以提高 Lf 的口服生物利用度。还讨论了现有局限性和未来研究的范围。
