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已发表论文
基于 pH 敏感 PAE-g -MPEG- 胆固醇嵌段共聚物的自组装胶束，用于抗癌药物递送
Authors Zhang CY, Xiong D, Sun Y, Zhao B, Lin WJ, Zhang LJ
Published Date October 2014 Volume 2014:9(1) Pages 4923—4933
DOI http://dx.doi.org/10.2147/IJN.S69493
Received 16 June 2014, Accepted 15 August 2014, Published 23 October 2014
Approved for publication by Dr Lei Yang
Abstract: A novel amphiphilic triblock pH-sensitive poly(β -amino ester)-g -poly(ethylene glycol) methyl ether-cholesterol (PAE-g -MPEG-Chol) was designed and synthesized via the Michael-type step polymerization and esterification condensation method. The synthesized copolymer was determined with proton nuclear magnetic resonance and gel permeation chromatography. The grafting percentages of MPEG and cholesterol were determined as 10.93% and 62.02%, calculated from the area of the characteristic peaks, respectively. The amphiphilic copolymer was confirmed to self-assemble into core/shell micelles in aqueous solution at low concentrations. The critical micelle concentrations were 6.92 and 15.14 mg/L at pH of 7.4 and 6.0, respectively, obviously influenced by the changes of pH values. The solubility of pH-responsive PAE segment could be transformed depending on the different values of pH because of protonation–deprotonation of the amino groups, resulting in pH sensitivity of the copolymer. The average particle size of micelles increased from 125 nm to 165 nm with the pH decreasing, and the zeta potential was also significantly changed. Doxorubicin (DOX) was entrapped into the polymeric micelles with a high drug loading level. The in vitro DOX release from the micelles was distinctly enhanced with the pH decreasing from 7.4 to 6.0. Toxicity testing proved that the DOX-loaded micelles exhibited high cytotoxicity in HepG2 cells, whereas the copolymer showed low toxicity. The results demonstrated how pH-sensitive PAE-g -MPEG-Chol micelles were proved to be a potential vector in hydrophobic drug delivery for tumor therapy.
Keywords: micelle, pH-sensitive, cholesterol,
poly(β -amino ester), drug delivery
