Amphiphilic oligomer-based micelles as cisplatin nanocarriers for cancer therapy
Xiuxiu Qi,ab Najun Li,*a （李娜君） Hongwei Gu,a Yujie Xu,c Ying Xu,c Yang Jiao,c Qingfeng Xu,a Hua Lia and Jianmei Lu*a（路建美）
a Jiangsu Key Laboratory of Advanced Functional Polymer Design and Application, College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou, China
b Changzhou Institute of Engineering Technology, Changzhou, China
c Medical College of Radiation Medicine and Protection, Soochow University, Suzhou, China
Nanoscale 2013, 5, 8925-8929.
Polymeric micelles ( 10 nm) have been prepared from the amphiphilic oligomer comprising oligomeric polystyrene as the hydrophobic inner core and half of EDTA (–N(CH2COOH)2) as the hydrophilic outermost shell. After chelating cisplatin with –N(CH2COOH)2 in water, polymeric micelles containing Pt on the spherical surface have been easily obtained. Since the chelate group is introduced into the amphiphilic oligomer as the terminal group by a RAFT agent, the chelation of cisplatin with PS(COOH)2 is almost stoichiometric. The drug carrier based on PS(COOH)2 showed a high loading efficiency (>70%) towards cisplatin. The release of the therapeutic Pt from the cisplatin-loaded composites (PS(COOH)2–Pt) triggered under weak acidic conditions resulted in good Pt-release and accumulation in tumor cells. Both in vitro and in vivo, the chelated cisplatin inhibited Sk-Br3 cancer more effectively than the intact cisplatin does. Furthermore, neither PS(COOH)2 nor PS(COOH)2–Pt showed obvious systematic toxicity.
链接： //pubs.rsc.org/en/content/articlelanding/2013/nr/c3nr03262k#!divAbstract
