Fabrication of microwave-sensitized nanospheres of covalent organic framework with apatinib for tumor therapy  

作　　者：Qijun Du Jian Zou Zhongbing Huang Shimei Li Longfei Tan Xiangling Ren Guangfu Yin Yongfa Zheng Xianwei Meng 

机构地区：[1]College of Biomedical Engineering,Sichuan University,Chengdu 610065,China [2]Laboratory of Controllable Preparation and Application of Nanomaterials,CAS Key Laboratory of Cryogenics,Technical Institute of Physics and Chemistry,Chinese Academy of Sciences,Beijing 100190,China [3]Sichuan Kangcheng Biotechnology Co.,Ltd.,Chengdu 610041,China [4]Department of Oncology,Renmin Hospital of Wuhan University,Wuhan 430060,China

出　　处：《Chinese Chemical Letters》2023年第5期427-432,共6页中国化学快报（英文版）

基　　金：supported by the National Key Research and Development Program of China(No.2018YFC1106800);National Natural Science Foundation of China(No.81703035);Sichuan Science&Technology Program(No.2020YFSY0018)。

摘　　要：A new nanocomposite of hollow covalent organic framework(COF)conjugated with the apatinib(AP)and loading microwave-sensitizer(ionic liquid,IL)was prepared by layer by layer(LBL)method and hyaluronic acid(HA)coating,named as [e-mail] loading rate in COF hollow-spheres(~30 nm shell thickness)was~40.3%,due to the interactions of hydrogen andπ-πbonds between AP and COF shell,and acidic environment destroyed COF structure,promoting AP release.Microwave sensitization of loaded IL in COF hollow-spheres could enhance the microwave heat-effect,and combined AP therapeutic ability,leading to their higher inhibitation on tumor,due to targeting ability of HA and the local release of apatinib.88.9%of inhibition rate of COF-AP-IL@HA under microwave on the in vivo tumor was significantly higher than those without microwave(12.3%)and COF-IL@HA with microwave(37.5%),indicating a synergism of sensitized microwave hyperthermia and AP therapy on the reduced expression of VEGF via the downregulation pathway of hypoxia inducible factor.These results indicated that COF-AP-IL@HA was potential to the application in the combination therapy of tumor of the sensitized microwave hyperthermia and apatinib.

关 键 词：Covalent organic framework ANTIANGIOGENESIS Tumor therapy Microwave hyperthermia Hollow spheres 

分 类 号：R730.5[医药卫生—肿瘤] TB383.1[医药卫生—临床医学]