Emulsion interfacial polymerization of anticancer peptides:fabricating polypeptide nanospheres with high drug-loading efficiency and enhanced anticancer activity  

作　　者：Jinpeng Yang Hua Wang Zihe Yin Shuai Zhang Jiang-Fei Xu Xi Zhang 

机构地区：[1]Key Lab of Organic Optoelectronics&Molecular Engineering,Department of Chemistry,Tsinghua University,Beijing 100084,China

出　　处：《Science China Chemistry》2022年第11期2252-2259,共8页中国科学（化学英文版）

基　　金：financially supported by the Ministry of Science and Technology of China(2021YFA1501600,2018YFA0208900);the National Natural Science Foundation of China(21821001);the Strategic Priority Research Program of Chinese Academy of Sciences(XDB36000000)。

摘　　要：The development of drug delivery systems with high drug-loading efficiency, kinetic stability against dilution, as well as enhanced anticancer activity is of crucial importance to the fields of self-assembly and nanomedicine. Herein, we propose a strategy where the anticancer peptide acts as water-soluble monomer to directly participate in emulsion interfacial polymerization for fabricating polypeptide nanospheres. The constructed polypeptide nanospheres hold a high drug loading efficiency of 77%, and can be stably dispersed in highly diluted aqueous solutions. The acid-labile amide linkage in polypeptide nanospheres can be hydrolyzed in tumor acidic environments, thus releasing anticancer peptides selectively. The polypeptide nanospheres achieve significantly enhanced anticancer activity against HCT116 cells in vitro and in vivo through improved mitochondrial and membrane disruption. In addition, its side effects on normal cells can be reduced significantly. It is highly anticipated that more kinds of anticancer drug candidates or anticancer drugs can be applied to fabricate polymeric nanomedicines with improved anticancer activity through this strategy.

关 键 词：emulsion interfacial polymerization drug delivery anticancer peptide self-assembly acidity-responsive 

分 类 号：TQ460.4[化学工程—制药化工] TQ316.334[一般工业技术—材料科学与工程] TB383.1