pH-sensitive Nanoparticles for High Loading and Efficient Delivery of Doxorubicin  

作　　者：鲁孟丽 黄丽华 ZHAN Siwen LI Juncan QIU Tong YANG Mengjia LI Jie TONG Miao ZHANG Xueqiong 施川 LU Mengli;HUANG Lihua;ZHAN Siwen;LI Juncan;QIU Tong;YANG Mengjia;LI Jie;TONG Miao;ZHANG Xueqiong;SHI Chuan(School of Chemistry,Chemical Engineering and Life Sciences,Wuhan University of Technology,Wuhan,430070,China;Tongji Medical College,Huazhong University of Science and Technology,Wuhan,430030,China;Wuhan Aimin Pharmaceutical Co.Ltd,Ezhou,436070,China;Hubei Li Shizhen Pharmaceutical Research Co.Ltd,Ezhou,436070,China)

机构地区：[1]School of Chemistry,Chemical Engineering and Life Sciences,Wuhan University of Technology,Wuhan,430070,China [2]Tongji Medical College,Huazhong University of Science and Technology,Wuhan,430030,China [3]Wuhan Aimin Pharmaceutical Co.Ltd,Ezhou,436070,China [4]Hubei Li Shizhen Pharmaceutical Research Co.Ltd,Ezhou,436070,China

出　　处：《Journal of Wuhan University of Technology(Materials Science)》2023年第4期929-937,共9页武汉理工大学学报（材料科学英文版）

基　　金：Funded by the Industrial Technology Research Institute of Hubei Provincial Department of Science and Technology(No.2020DEB012);the Hubei Provincial Department of Science and Technology Support Enterprise Technology Innovation Development Project(No.2021BAB119)。

摘　　要：An acid-sensitive delivery system based on acylhydrazone bond was developed for high loading and efficient delivery of doxorubicin.Doxorubicin(DOX)was covalently combined with dihydrazide adipate to form acid-sensitive hydrazone bond based on Schiff base reaction,then the intermediate was covalently combined with carboxymethyl chitosan through amide bond to form polymeric prodrugs,and nanoparticles were formed through self-assembling.Moreover,the structural and particle properties of CMCS-ADH-DOX were characterized by ultraviolet visible near infrared spectrophotometry(UV),nuclear magnetic resonance spectroscopy(^(1)H-NMR),fourier transform infrared spectroscopy(FT-IR),dynamic light scattering(DLS),and transmission electron microscopy(TEM).The mean diameter of the self-assembled nanoparticles is 165 nm,while the morphology is a relatively uniform spherical shape.Moreover,these DOXloaded nanoparticles showed pH-triggered drug release behavior.Compared with free DOX,CAD NPs showed lower toxic side effects in L929 cells and similar toxicity in 4T1 cells.The experimental results indicate that the CMCS-ADH-DOX nanoparticles may be used as an acid-sensitive targeted delivery system with good application prospect for cancer.

关 键 词：NANOPARTICLES acylhydrazone bond polymeric prodrug acid-sensitive 

分 类 号：TQ460.4[化学工程—制药化工] TB383.1[一般工业技术—材料科学与工程]