Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; University of Chinese Academy of Sciences, Beijing 100049, China.
Center for Drug Delivery System, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Carbohydr Polym. 2018 Jun 15;190:23-30. doi: 10.1016/j.carbpol.2018.02.044. Epub 2018 Feb 21.
Cyclodextrins nanosponges (CD-NSPs) are highly microporous crosslinked polymers with potential applications in the delivery of small and macro-molecular therapeutic agents. Despite the potent host-guest inclusion property, their inherent lack of cellular binding ability has limited applications in drug delivery. Herein, we functionalized the surface of β-cyclodextrin nanosponge (β-CD-NSP) with cholesterol, which is endogenous physiological molecules, widely distributed in all cells, and responsible for cell interactions and protein binding. The surface grafting of synthesized β-CD-NSP was confirmed with spectroscopic, microscopic, thermogravimetric, and chromatographic techniques. Moreover, β-CD-NSP was found to be safe in cytotoxicity assay. Doxorubicin (Dox) was selected as a model drug for drug adsorption study of cholesterol hydrogen succinate (CHS) grafted β-CD-NSP. The cellular uptake of NSP was found to be enhanced after CHS modification confirmed by confocal laser scanning microscopy (CLSM). Thus, proposed CHS modified β-CD-NSP system could be used as a site-specific drug delivery carrier.
环糊精纳米海绵（CD-NSPs）是一种具有微孔结构的交联聚合物，在小分子和大分子治疗剂的递送中具有潜在的应用。尽管具有很强的主客体包合性能，但由于其缺乏固有细胞结合能力，在药物递送中的应用受到限制。在此，我们用胆固醇对β-环糊精纳米海绵（β-CD-NSP）的表面进行功能化修饰，胆固醇是内源性生理分子，广泛分布于所有细胞中，负责细胞相互作用和蛋白质结合。合成的β-CD-NSP 的表面接枝通过光谱、显微镜、热重分析和色谱技术得到了证实。此外，细胞毒性测定表明β-CD-NSP 是安全的。阿霉素（Dox）被选为胆固醇琥珀酸氢（CHS）接枝β-CD-NSP 的药物吸附研究的模型药物。通过共聚焦激光扫描显微镜（CLSM）证实，CHS 修饰后 NSP 的细胞摄取能力增强。因此，所提出的 CHS 修饰的β-CD-NSP 系统可用作靶向药物递送载体。
