多肽、蛋白质、核苷酸及质粒等复杂高分子的粘膜释放给药是当前最受关注的研究课题之一。壳聚糖作为一种天然高分子多糖，已经被认为是一种最具希望的高分子药物的跨膜输送载体。而壳聚糖纳米微粒是主要的载体形式之一。本文综述了壳聚糖纳米微粒药物载体的制备方法以及输送高分子药物的作用机制。现已表明壳聚糖可通过离子交联、共价交联、沉淀析出、大分子复合及自组装等方法获取负载大分子药物的壳聚糖纳米胶体粒子。结尾阐述了这种新型载药系统的存在的问题及应用前景。

Mucosal delivery of complex molecules such as peptides, proteins, oligonucleotides, and plasmids is of increasing interest in recent years. Using a hydrophilic polysaccharide (chitosan) as colloidal carriers has become a promising alternative for improving the transport of such macromolecules across biological surfaces. This article reviews the approaches to prepare drug-loaded nanoparticles derived from chitosan and the action mechanism of their efficacy in improvement of the transport of the associated molecule through biological surfaces. Chitosan can form colloidal particles and entrap macromolecules through a number of mechanisms, including ionic crosslinking, covalent crosslinking, desolvating, supramolecular complexation, or self-assemblies. The potential applications and prospects of these new systems for mucosal delivery of macromolecules are also highlighted.