Delivery of active DACH-Pt anticancer species by biodegradable amphiphilic polymers using thiol-ene radical addition.
A biodegradable and amphiphilic copolymer, mPEG-b-P(LA-co-MAC/TMA) that contains pendant 1,2-bidentate carboxyl groups is synthesized by thiol-ene radical addition and is further used to chelate with the active anticancer species (DACH-Pt) of oxaliplatin to form an mPEG-b-P(LA-co-MAC/TMA-Pt-DACH) complex. The polymer platinum complex can self-assemble into micelles. In vitro studies show that the DACH-Pt micelles display enhanced or comparable cytotoxicity against SKOV-3 and MCF-7 cancer cells, while they show reduced toxicity to HeLa cells compared with oxaliplatin.
State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China.
Haihua
H
Xiao
Dongfang
D
Zhou
Shi
S
Liu
Ruogu
R
Qi
Yonghui
Y
Zheng
Yubin
Y
Huang
Xiabin
X
Jing
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000138:chemical synthesis*; D006801:Humans; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy; D008823:Micelles; D009944:Organoplatinum Compounds / Q000737:chemistry* / Q000494:pharmacology; D000077150:Oxaliplatin; D011091:Polyesters / Q000138:chemical synthesis*; D011092:Polyethylene Glycols / Q000138:chemical synthesis*; D013439:Sulfhydryl Reagents / Q000737:chemistry*; D013501:Surface-Active Agents / Q000138:chemical synthesis*
D000970:Antineoplastic Agents; D004337:Drug Carriers; D008823:Micelles; D009944:Organoplatinum Compounds; D011091:Polyesters; D013439:Sulfhydryl Reagents; D013501:Surface-Active Agents; D000077150:Oxaliplatin; D011092:Polyethylene Glycols