基于喜树碱-环糊精主客体作用的超分子纳米药物的制备  

Preparation of Supramolecular Nanomedicine Based on Host-Guest Interaction Between Camptothecin and Cyclodextrin

作　　者：曹辰辉 孙长瑞 姚锡矿 CAO Chenhui;SUN Changrui;YAO Xikuang(Anhui Sholon New Material Technology Company Limited,Chuzhou 239500,China;School of Flexible Electronics(Future Technology),Nanjing Tech University,Nanjing 211800,China)

机构地区：[1]安徽秀朗新材料科技有限公司,滁州239500 [2]南京工业大学柔性电子(未来技术)学院,江苏南京211800

出　　处：《化学反应工程与工艺》2024年第4期333-341,369,共10页Chemical Reaction Engineering and Technology

基　　金：江苏省科技厅自然科学基金项目(BK20200709);江苏省教育厅面上项目(20KJB430031)。

摘　　要：为改善喜树碱药物的水溶性差和在生理条件下容易开环导致抗肿瘤效果显著降低的问题,本工作设计并制备了基于喜树碱和β-环糊精主客体相互作用的自组装超分子纳米药物,并探索了不同加水速度和聚喜树碱的聚合度对自组装纳米药物构建的影响。结果表明:通过控制单体和引发剂的比例,得到聚合度分别为5,10和20的聚喜树碱;同时,设计并合成了带有叠氮基的β-环糊精,利用高效的Click反应将环糊精接枝到透明质酸的末端,从而得到末端接枝β-环糊精的透明质酸。最后,通过喜树碱和环糊精的主客体相互作用,自组装得到超分子纳米药物。自组装水滴加速度慢有利于形成分散均匀的颗粒。这为今后纳米药物的设计提供了一定的借鉴意义。To improve the poor water solubility of camptothecin and prevent the significant reduction in its anti-cancer effects caused by ring-opening under physiological conditions,a self-assembled supramolecular nanomedicine based on the host-guest interaction of camptothecin andβ-cyclodextrin was designed and prepared in this work,and the effects of different water addition rates and polymerization degree of camptothecin on the construction of self-assembled nanomedicine were explored.The results showed that polycamptothecin with polymerization degrees of 5,10,and 20 was obtained by controlling the ratio of monomers and initiators.At the same time,β-cyclodextrin with azide group was designed and synthesized,and the cyclodextrin was grafted to the end of hyaluronic acid by efficient Click reaction.In the end,supramolecular nanomedicine was self-assembled by the host-guest interaction between camptothecin and cyclodextrin.The slow acceleration of water droplets is conducive to self-assembly to form dispersed and uniform particles.It provides some reference significance for the design of nanomedicine in the future.

关 键 词：喜树碱 纳米药物 透明质酸 主客体相互作用 

分 类 号：TQ079[化学工程] TQ463.5