Tumor acid microenvironment-activated self-targeting&splitting gold nanoassembly for tumor chemo-radiotherapy

作     者：Xiaomin Li Licheng Yu Chuangnian Zhang Xiaoyan Niu Mengjie Sun Zichao Yan Wei Wang Zhi Yuan 

作者机构：Key Laboratory of Functional Polymer Materials of Ministry of EducationCollege of ChemistryNankai UniversityTianjin300071China Tianjin Key Laboratory of Biomaterial ResearchBiomedical Barriers Research CenterInstitute of Biomedical EngineeringChinese Academy of Medical Science&Peking Union Medical CollegeTianjin300192China Collaborative Innovation Center of Chemical Science and EngineeringNankai UniversityTianjin300071China 

出 版 物：《Bioactive Materials》 (生物活性材料（英文）)

年 卷 期：2022年第7卷第1期

页      面：377-388页

核心收录：

学科分类：0831[工学-生物医学工程（可授工学、理学、医学学位）] 0710[理学-生物学] 1002[医学-临床医学] 0805[工学-材料科学与工程（可授工学、理学学位）] 100214[医学-肿瘤学] 0836[工学-生物工程] 10[医学] 

基　　金：This study is dedicated to 100th anniversary of Chemistry at Nankai University.This work was supported by the National Natural Science Foundation of China(Grant 52073147,51773096,51433004,32071342) Specific Program for High-Tech Leader&Team of Tianjin Government,Tianjin innovation and Promotion Plan Key Innovation Team of Immunoreactive Biomaterials.We appreciate Prof.Qiang Wu at Nankai University for help with the characterization of materials and Dr.Ding Yuxun for help with characterization of penetration 

主　　题：Gold nanoassembly Disassemble Penetration Self-target Chemo-radiotherapy 

摘      要：Low accumulation and penetration of nanomedicines in tumor severely reduce therapeutic ***,a pH-responsive gold nanoassembly is designed to overcome these *** glycol linked raltitrexed(RTX,target ligand and chemotherapy drug)and two tertiary amine molecules(1-(2-aminoethyl)pyrrolidine and N,N-dibutylethylenediamine)are modified on the surface of the 6-nm gold nanoparticles by lipoic acid to form gold nanoassembly defined as Au-NNP(RTX).The Au-NNP(RTX)nanoassembly could remain at about 160 nm at the blood circulation(pH 7.4),while split into 6-nm gold nanoparticles due to tertiary amine protonation at tumor extracellular pH(pH 6.8).This pH-responsive disassembly behavior endows Au-NNP(RTX)better tumor tissue permeability through the better diffusion brought by the size ***,after disassembly,more RTXs on the surface of gold nanoparticles are exposed from the shielded state of assembly along with 2.25-fold augment of cellular uptake *** importantly,the results show that Au-NNP(RTX)possesses of high tumor accumulation and effective tumor penetration,thereby enhancing the tumor chemo-radiotherapy efficiency.