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Effects of copolymer component on the properties of phosphorylcholine micelles

Authors Wu Z, Cai M, Cao J, Zhang J, Luo X

Received 26 July 2016

Accepted for publication 8 December 2016

Published 12 January 2017 Volume 2017:12 Pages 487—500

DOI https://doi.org/10.2147/IJN.S118197

Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 3

Editor who approved publication: Dr Linlin Sun


Zhengzhong Wu,1 Mengtan Cai,1 Jun Cao,2 Jiaxing Zhang,1 Xianglin Luo1,3

1College of Polymer Science and Engineering, 2National Engineering Research Center for Biomaterials, 3State Key Laboratory of Polymer Materials Engineering, Sichuan University, Chengdu, People’s Republic of China

Abstract: Zwitterionic polymers have unique features, such as good compatibility, and show promise in the application of drug delivery. In this study, the zwitterionic copolymers, poly(ε-caprolactone)-b-poly(2-methacryloyloxyethyl phosphorylcholine) with disulfide (PCL-ss-PMPC) or poly(ε-caprolactone)-b-poly(2-methacryloyloxyethyl phosphorylcholine) or without disulfide (PCL-PMPC) and with different block lengths in PCL-ss-PMPC, were designed. The designed copolymers were obtained by a combination of ring-opening polymerization and atom transferring radical polymerization. The crystallization properties of these polymers were investigated. The micelles were prepared based on the obtained copolymers with zwitterionic phosphorylcholine as the hydrophilic shell and PCL as the hydrophobic core. The size distributions of the blank micelles and the doxorubicin (DOX)-loaded micelles were uniform, and the micelle diameters were <100 nm. In vitro drug release and intracellular drug release results showed that DOX-loaded PCL-ss-PMPC micelles could release drugs faster responding to the reduction condition and the intracellular microenvironment in contrast to PCL-PMPC micelles. Moreover, in vitro cytotoxicity evaluation revealed that the designed copolymers possessed low cell toxicity, and the inhibiting effect of DOX-loaded phosphorylcholine micelles to tumor cells was related to the components of these copolymers. These results reveal that the reduction-responsive phosphorylcholine micelles with a suitable ratio of hydrophilic/hydrophobic units can serve as promising drug carriers.

Keywords: zwitterionic, reduction-sensitive, disulfide, phosphorylcholine

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