Division of Bioengineering, Faculty of Engineering, National University of Singapore (NUS), 7 Engineering Drive 1, Singapore, 117574, Singapore.
Adv Biochem Eng Biotechnol. 2011;125:207-49. doi: 10.1007/10_2010_91.
Supramolecular polymers based on cyclodextrins (CDs) have inspired interesting and rapid developments as novel biomaterials in a broad range of drug and gene delivery applications, due to their low cytotoxicity, controllable size, and unique architecture. This review will summarize the potential applications of polyrotaxanes in the field of drug delivery and gene delivery. Generally, cyclodextrin-based biodegradable polypseudorotaxane hydrogels could be used as a promising injectable drug delivery system for sustained and controlled drug release. Temperature-responsive, pH-sensitive, and controllable hydrolyzable polyrotaxane hydrogels have attracted much attention because of their controllable properties, and the self-assembly micelles formed by amphiphilic copolymer threaded with CDs could be used as a carrier for controlled and sustained drug release. Polyrotaxanes with drug or ligand conjugated CDs threaded on a polymer chain with a biodegradable end group could be useful for controlled and multivalent targeted delivery. In the field of gene delivery, cationic polyrotaxanes consisting of multiple OEI-grafted CDs threaded on a block copolymer chain are attractive non-viral gene carries due to the strong DNA-binding ability, low cytotoxicity, and high gene delivery capability. Furthermore, cytocleavable end-caps were introduced in the polyrotaxane systems in order to ensure efficient endosomal escape for intracellular trafficking of DNA. The development of the supramolecular approach using CD-containing polyrotaxanes is expected to provide a new paradigm for biomaterials.
基于环糊精（CDs）的超分子聚合物因其低细胞毒性、可控制的尺寸和独特的结构，在广泛的药物和基因传递应用中作为新型生物材料引起了人们的兴趣和快速发展。本文综述了聚轮烷在药物传递和基因传递领域的潜在应用。一般来说，基于 CD 的可生物降解的假轮烷水凝胶可用作有前途的可注射药物传递系统，以实现持续和控制药物释放。温度响应、pH 敏感和可控水解聚轮烷水凝胶因其可控特性而受到关注，由两亲性共聚物与 CD 螺旋形成的自组装胶束可用作控制和持续药物释放的载体。具有药物或配体共轭 CD 的聚轮烷，其 CD 链上接有可生物降解的端基聚合物链，可用于控制和多价靶向传递。在基因传递领域，由多个 OEI 接枝的 CD 串在嵌段共聚物链上的阳离子聚轮烷由于具有强 DNA 结合能力、低细胞毒性和高基因传递能力，是有吸引力的非病毒基因载体。此外，在聚轮烷体系中引入可切割的细胞内溶酶体帽，以确保 DNA 在内体逃逸中的有效细胞内运输。使用含 CD 的聚轮烷的超分子方法的发展有望为生物材料提供新的范例。
