黏液穿透纳米递送系统克服口服吸收黏液屏障的研究进展

Progress in intestinal mucus penetrating particles for overcoming the oral absorption mucus barriers

近年来,蛋白多肽类生物大分子药物受到了越来越多的关注,然而其口服生物利用度低,解决这一问题的关键方法是采用纳米递送系统。纳米递送系统口服后必须克服多重屏障才可能被有效吸收,其中一个对吸收有重要影响的屏障是黏液屏障。本文针对肠道黏液的性质特点,综述了克服口服吸收屏障的黏液穿透纳米递送系统研究进展,探讨了黏液穿透纳米载体的研究方向和取得的成果,包括聚乙二醇(PEG)、N-(2-羟丙基)甲基丙烯酰胺共聚物(pHPMA)、两性离子以及基于仿生功能化概念的纳米递送系统。本文旨在为克服口服吸收屏障的制剂研发、应用提供参考。

Oral administration of biological macromolecule drugs is of great significance in pharmaceutical research. However,oral administration of biodrugs is restricted due to its low bioavailability. The key way to solve this problem is to use nano-delivery systems. Nano-delivery systems must overcome multiple barriers after oral administration. One of the barriers that has important impact on absorption is the mucus barrier. In this paper,a large number of research was reviewed. The intestinal mucus penetrating particles are mainly based on polyethylene glycol,N-(2-hydroxypropyl) methacrylamide(HPMA) polymer(pHPMA) derivatives,zwitterion and biomimetic functionalization. This paper aims to provide some references for the research,development and application of pharmaceutical preparations which can overcome the oral absorption barriers.