title: Effects of copolymer component on the properties of phosphorylcholine micelles.
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.
authors.affiliation: College of Polymer Science and Engineering.
authors.forename: Zhengzhong
authors.initials: Z
authors.lastname: Wu
authors.affiliation: College of Polymer Science and Engineering.
authors.forename: Mengtan
authors.initials: M
authors.lastname: Cai
authors.affiliation: National Engineering Research Center for Biomaterials.
authors.forename: Jun
authors.initials: J
authors.lastname: Cao
authors.affiliation: College of Polymer Science and Engineering.
authors.forename: Jiaxing
authors.initials: J
authors.lastname: Zhang
authors.affiliation: College of Polymer Science and Engineering; State Key Laboratory of Polymer Materials Engineering, Sichuan University, Chengdu, People's Republic of China.
authors.forename: Xianglin
authors.initials: X
authors.lastname: Luo
mesh_terms: D000818:Animals; D002152:Calorimetry, Differential Scanning; D016923:Cell Death / Q000187:drug effects; D004317:Doxorubicin / Q000494:pharmacology; D016503:Drug Delivery Systems; D065546:Drug Liberation; D004705:Endocytosis / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans; D042541:Intracellular Space / Q000378:metabolism; D008689:Methacrylates / Q000737:chemistry; D051379:Mice; D008823:Micelles; D010316:Particle Size; D010767:Phosphorylcholine / Q000031:analogs & derivatives / Q000737:chemistry*; D011091:Polyesters / Q000737:chemistry; D058105:Polymerization; D011108:Polymers / Q000138:chemical synthesis / Q000737:chemistry*; D011109:Polymethacrylic Acids / Q000737:chemistry; D066244:Proton Magnetic Resonance Spectroscopy; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D008689:Methacrylates; D008823:Micelles; D011091:Polyesters; D011108:Polymers; D011109:Polymethacrylic Acids; C115766:poly(2-methacryloyloxyethyl-phosphorylcholine); D010767:Phosphorylcholine; C016240:polycaprolactone; C070638:2-methacryloyloxyethyl phosphorylcholine; D004317:Doxorubicin
keywords: disulfide; phosphorylcholine; reduction-sensitive; zwitterionic