title: pH and redox-responsive mixed micelles for enhanced intracellular drug release.
abstract: In order to prepare pH and redox sensitive micelles, amphiphilic copolymers of poly (epsilon-caprolactone)-b-poly(2-(diethylamino) ethyl methacrylate) (PCL-PDEA) and disulfide-linked poly(ethyl glycol)-poly(epsilon-caprolactone) (mPEG-SS-PCL) were synthesized. The double-sensitive micelles were prepared simply by solvent-evaporating method with the mixed two copolymers. The pH sensitivity of the mixed micelles was confirmed by the change of micelle diameter/diameter distribution measured by dynamic lighting scattering (DLS) and the redox sensitivity of the mixed micelles was testified by the change of micellar morphous observed by scanning electron microscope (SEM). In vitro drug release showed that drug-loaded mixed micelles (mass ratio 5:5) could achieve above 90% of drug release under low pH and reducing condition within 10h. Moreover, the drug-loaded mixed micelles (mass ratio 5:5) showed the largest cellular toxicity compared with other drug-loaded micelles, while blank mixed micelles exhibited no toxicity. These results meant that the mixed micelles composed by the two amphiphilic copolymers can enhance intracellular drug release. It is concluded that the newly developed mixed micelles can serve as a potential drug delivery system for anticancer drugs.
authors.affiliation: College of polymer science and engineering of Sichuan University, Chengdu 610065, China.
authors.forename: Mengtan
authors.initials: M
authors.lastname: Cai
authors.affiliation: College of polymer science and engineering of Sichuan University, Chengdu 610065, China.
authors.forename: Kun
authors.initials: K
authors.lastname: Zhu
authors.affiliation: College of polymer science and engineering of Sichuan University, Chengdu 610065, China.
authors.forename: Yongbin
authors.initials: Y
authors.lastname: Qiu
authors.affiliation: School of life Science and Engineering, Southwest Jiaotong University, Chengdu 610031, China.
authors.forename: Xinrong
authors.initials: X
authors.lastname: Liu
authors.affiliation: College of polymer science and engineering of Sichuan University, Chengdu 610065, China.
authors.forename: Yuanwei
authors.initials: Y
authors.lastname: Chen
authors.affiliation: College of polymer science and engineering of Sichuan University, Chengdu 610065, China; State Key Laboratory of Polymer materials and engineering of China (Sichuan University), Chengdu 610065, China. Electronic address: luoxl@scu.edu.cn.
authors.forename: Xianglin
authors.initials: X
authors.lastname: Luo
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D003474:Curcumin / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D016503:Drug Delivery Systems; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008823:Micelles; D015394:Molecular Structure; D010084:Oxidation-Reduction; D011108:Polymers / Q000138:chemical synthesis / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013501:Surface-Active Agents / Q000138:chemical synthesis / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D008823:Micelles; D011108:Polymers; D013501:Surface-Active Agents; D003474:Curcumin
keywords: Curcumin; Drug delivery; Dual response; Redox sensitive; pH Sensitive