Werle Martin, Takeuchi Hirofumi, Bernkop-Schnürch Andreas
Department of Drug Delivery Technology and Science, Laboratory of Pharmaceutical Engineering, Gifu Pharmaceutical University, 5-6-1 Mitahora-Higashi, Gifu 502-8585, Japan.
J Pharm Sci. 2009 May;98(5):1643-56. doi: 10.1002/jps.21550.
The cationic polysaccharide chitosan has been extensively studied for oral drug delivery. In recent years, chemically modified chitosans developed in order to improve the properties of chitosan for oral drug delivery have gained increasing attention. Representatives of these novel polymers are trimethyl-chitosans, thiolated chitosans, carboxymethyl chitosan and derivatives, hydrophobic chitosans, chitosan succinate and phthalate, PEGylated chitosans and chitosan-enzyme inhibitor conjugates. Besides their use for oral delivery of therapeutic peptides and proteins, they have recently been evaluated regarding their potential for the delivery of other substance classes, including genes and efflux pump substrates. Within the current review, various modified chitosan derivatives, their properties and synthesis are discussed.
阳离子多糖壳聚糖已被广泛研究用于口服给药。近年来,为改善壳聚糖用于口服给药的性能而开发的化学修饰壳聚糖受到了越来越多的关注。这些新型聚合物的代表有三甲基壳聚糖、硫醇化壳聚糖、羧甲基壳聚糖及其衍生物、疏水壳聚糖、壳聚糖琥珀酸酯和邻苯二甲酸酯、聚乙二醇化壳聚糖以及壳聚糖-酶抑制剂缀合物。除了用于口服递送治疗性肽和蛋白质外,最近还对它们递送其他物质类别(包括基因和外排泵底物)的潜力进行了评估。在本综述中,讨论了各种修饰的壳聚糖衍生物、它们的性质和合成方法。