“多胺-环糊精-量子点”纳米药物转运系统的设计及生物活性研究

项目名称： “多胺-环糊精-量子点”纳米药物转运系统的设计及生物活性研究

项目编号： No.U1204201

项目类型： 联合基金项目

立项/批准年度： 2013

项目学科： 无机化学

项目作者： 赵美霞

作者单位： 河南大学

项目金额： 30万元

中文摘要： 抗肿瘤药物的运输系统与控制释放是抗癌药物新技术发展的重要研究思路。半导体量子点(QDs)，由于其光学性质较好，在生物探针和药物载体等方面极为有用，而多胺是一类集肿瘤靶向和正电荷于一身的有机化合物。本项目旨在设计合成一系列多胺有机配体修饰的环糊精功能化的量子点 (包括CdSe、CdSe/CdS、CdSe/ZnSe等) 纳米药物转运系统，将药物阿霉素装载于环糊精空腔内，而将mdr1 siRNA吸附于带正电荷的多胺有机配体上，然后进行系统性的细胞及分子生物学实验研究，考察单载药和联合载药时体外、体内抑瘤效果，建立全面的构效关系。由于多胺本身具有肿瘤靶向性，所以不需要再用其他的靶向分子来修饰转运系统，这就使得我们的靶向纳米药物转运系统设计更简单化。此项研究对阐明靶向药物传输以及纳米药物转运系统的设计有重要意义，也可为更好地设计靶向药物以及纳米药物转运系统奠定基础。

中文关键词： 量子点；多胺；氨基酸；环糊精；纳米药物转运系统

英文摘要： The transport system and the control release of anti-cancer drugs is a new important research technologies for cancer drugs. Semiconductor quantum dots (QDs) show good optical properties, so the QDs were more and more applied in bioprobes and nanocarrier. Polyamine is a kind of organic compounds with positive charge and the tumor targeting. In this project, we aimed to design a series of tumor targeted polyamine modified cyclodextrins functionalized inorganic quantum dots (CdSe、CdSe/CdS、CdSe/ZnSe, etc.) delivery drug system. The doxorubicine drug will be carried on cyclodextrins cavity, and mdr1 siRNA will adsorb on positively charged in organic ligands polyamine. Then the antitumor effect in vitro and in vivo toxicity were investigated by the systematic cell and molecular biology experiment, and set up the comprehensive structure-activity relationship. Because polyamine itself is the tumor targeted molecule, so don''t need to use other targeted molecular to modify the carrier, this will make the design of targeted nano drug carrier more simple. This project study would has an important meaning to clarify targeted drugs transmission and delivery drug system design, and also can lay the foundation for better design targeted drugs and delivery drug system.

英文关键词： Quantum dots；polyamine；amino acid；cyclodextrin；delivery nano-drug system