肿瘤靶向pH响应药物递送-成像体系的合成与控制释放研究  

Synthesis and controlled release of tumor-targeted pH-responsive drug delivery-imaging system

作　　者：施萍 曾贤伍[2] 何文涛 彭立聪 祁芊芊 袁建超[1] SHI Ping;ZENG Xianwu;HE Wentao;PENG Licong;QI Qianqian;YUAN Jianchao(Key Laboratory of Gansu Polymer Materials,College of Chemistry and Chemical Engineering,Northwest Normal University,Lanzhou 730070,Gansu,China;Department of Nuclear Medicine,Cancer Hospital Gansu Province,Lanzhou 730050,Gansu,China)

机构地区：[1]西北师范大学化学化工学院,甘肃省高分子材料重点实验室,甘肃兰州730070 [2]甘肃省肿瘤医院核医学科,甘肃兰州730050

出　　处：《化学研究》2019年第2期182-188,共7页Chemical Research

基　　金：国家自然科学基金(21364011; 20964003)

摘　　要：对聚烯丙基胺修饰合成了一种苯硼酸靶向的聚合物配体:聚烯丙基胺/马来酸酐-聚乙二醇-硫辛酸-苯硼酸(PAH/SA-PEG-LA-PBA),共轭作用在ZnO、CdTe/CdS量子点表面,连接抗癌药物阿霉素后形成苯硼酸靶向-示踪诊疗一体体系:ZnO、CdTe/CdS@(PAH/SA-PEG-LA-PBA)-DOX(量子点的荧光可示踪/显像药物递送过程),核磁共振(1H-NMR)测试表明成功合成了(PAH/SA-PEG-LA-PBA)聚合物,透射电镜(TEM)测得该体系呈规整球形且分布均匀,平均粒径约30nm;紫外-可见光谱(UV-Vis)和荧光谱图显示该体系具有ZnO、CdTe/CdS量子点的吸收峰,还出现了较强的荧光发射峰,由此说明了苯硼酸靶向的诊疗示踪一体体系的成功制得,负载阿霉素的纳米粒子的载药量为80%.体外释放研究表明,pH5.0时药物释放速度比pH7.4时快,48h后累计释放率达87.1%.因此,该pH响应性纳米颗粒作为抗癌药物载体具有潜在的应用价值.A phenylboronic acid-targeted polymer ligand was synthesized by modification of polyallylamine:polyallylamine/maleic anhydride-polyethylene glycol-lipoic acid-phenylboronic acid (PAH/SA-PEG-LA-PBA),which was conjugated to the surface of ZnO and CdTe/CdS quantum dots and connected with the anticancer drug doxorubicin to form a system of phenylborate targeting-trace diagnosis and treatment: ZnO,CdTe/CdS@(PAH/SA-PEG-LA-PBA)-DOX(fluorescence traceable/developing drug delivery process for quantum dots),nuclear magnetic resonance (1H-NMR) analysis showed that the (PAH/SA-PEG-LA-PBA) polymer was successfully synthesized.The system was spherical and uniform in distribution by TEM.The average particle size was about 30 nm,UV-Vis and the fluorescence spectrum shows that the system has characteristic absorption peaks of ZnO.CdTe/CdS quantum dots and a strong fluorescence emission peak appears,This shows the successful system of phenylboronic acid-targeted diagnosis and tracing integrated system,The drug loading of the doxorubicin-loaded nanoparticles was 80%,In vitro release studies showed that the drug release rate was faster at pH 5.0 than at pH 7.4,and the cumulative release rate was 87.1% after 48 h,Therefore,the pH responsive nanoparticle has potential application value as an anticancer drug carrier.

关 键 词：氧化锌、CdTe/CdS量子点 苯硼酸 阿霉素 PH敏感 

分 类 号：O632[理学—高分子化学]