Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences (UIPS), Utrecht University, P.O. Box 80082, 3508 TB Utrecht, The Netherlands.
Adv Drug Deliv Rev. 2010 Jan 31;62(1):59-82. doi: 10.1016/j.addr.2009.11.009. Epub 2009 Nov 16.
Therapeutic peptides/proteins and protein-based antigens are chemically and structurally labile compounds, which are almost exclusively administered by parenteral injections. Recently, non-invasive mucosal routes have attracted interest for administration of these biotherapeutics. Chitosan-based delivery systems enhance the absorption and/or cellular uptake of peptides/proteins across mucosal sites and have immunoadjuvant properties. Chitosan is a mucoadhesive polysaccharide capable of opening the tight junctions between epithelial cells and it has functional groups for chemical modifications, which has resulted in a large variety of chitosan derivatives with tunable properties for the aimed applications. This review provides an overview of chitosan-based polymers for preparation of both therapeutic peptides/protein and antigen formulations. The physicochemical properties of these carrier systems as well as their applications in protein and antigen delivery through parenteral and mucosal (particularly nasal and pulmonary) administrations are summarized and discussed.
治疗性肽/蛋白质和基于蛋白质的抗原是化学和结构不稳定的化合物，几乎专门通过肠胃外注射给药。最近，非侵入性黏膜途径引起了人们对这些生物治疗药物给药的兴趣。基于壳聚糖的递药系统增强了肽/蛋白质在黏膜部位的吸收和/或细胞摄取，并且具有免疫佐剂特性。壳聚糖是一种具有黏膜黏附性的多糖，能够打开上皮细胞之间的紧密连接，并且具有用于化学修饰的功能基团，这导致了具有可调节特性的大量壳聚糖衍生物，可用于预期的应用。本文综述了用于制备治疗性肽/蛋白质和抗原制剂的壳聚糖基聚合物。总结和讨论了这些载体系统的物理化学性质及其在通过肠胃外和黏膜（特别是鼻内和肺部）途径给药的蛋白质和抗原传递中的应用。
