Cui Jian, Wen Zhiwei, Zhang Wei, Wu Wei
School of Pharmacy, Guilin Medical University, Guilin 541199, China.
Pharmaceuticals (Basel). 2022 Aug 28;15(9):1072. doi: 10.3390/ph15091072.
The high physiology and low toxicity of therapeutic peptides and proteins have made them a hot spot for drug development in recent years. However, their poor oral bioavailability and unstable metabolism make their clinical application difficult. The bilayer membrane of liposomes provides protection for the drug within the compartment, and their high biocompatibility makes the drug more easily absorbed by the body. However, phospholipids-which form the membranes-are subjected to various digestive enzymes and mucosal adhesion in the digestive tract and disintegrate before absorption. Improvements in the composition of liposomes or modifying their surface can enhance the stability of the liposomes in the gastrointestinal tract. This article reviews the basic strategies for liposome preparation and surface modification that promote the oral administration of therapeutic polypeptides.
治疗性肽和蛋白质的高生理学活性和低毒性使其成为近年来药物开发的热点。然而,它们较差的口服生物利用度和不稳定的代谢使其临床应用困难。脂质体的双层膜为包裹在其中的药物提供保护,其高生物相容性使药物更易被机体吸收。然而,构成膜的磷脂在消化道中会受到各种消化酶的作用和黏膜黏附,在吸收前就会分解。改进脂质体的组成或修饰其表面可以提高脂质体在胃肠道中的稳定性。本文综述了促进治疗性多肽口服给药的脂质体制备和表面修饰的基本策略。