title: Drug-loaded pseudo-block copolymer micelles with a multi-armed star polymer as the micellar exterior.
abstract: Supramolecular constructed pseudo block copolymer micelles based on β-cyclodextrin terminated 4 and 7 armed star poly(N-vinylpyrrolidone) and adamantane terminated linear poly(ε-caprolactone) were prepared. The size, morphology, stability and protein adsorption were experimentally examined. The micelles with 7 armed PVP chains as the micellar exterior showed the lowest amount of protein adsorption and the best stability in media. When cabazitaxel, a new taxane, was loaded into the micelles, 14.4% drug loading content and 85% encapsulation efficacy were achieved. In vitro cytotoxicity studies demonstrated that the cabazitaxel-loaded micelles show significant cytotoxicity against drug-resistant A2780/T cell lines. Biodistribution studies showed that the micelles can almost double the content of cargo in tumor sites compared with the free cargo. In vivo antitumor activity examinations indicated that cabazitaxel-loaded micelles show superior antitumor activity over free paclitaxel and free cabazitaxel.
authors.affiliation: MOE Key Laboratory of High Performance Polymer Materials and Technology, and Department of Polymer Science & Engineering, College of Chemistry & Chemical Engineering, Nanjing University, Nanjing, 210093, P. R. China. jiangx@nju.edu.cn.
authors.forename: Chen
authors.initials: C
authors.lastname: Xie
authors.forename: Peng
authors.initials: P
authors.lastname: Zhang
authors.forename: Zhengkui
authors.initials: Z
authors.lastname: Zhang
authors.forename: Chenchen
authors.initials: C
authors.lastname: Yang
authors.forename: Jialiang
authors.initials: J
authors.lastname: Zhang
authors.forename: Wei
authors.initials: W
authors.lastname: Wu
authors.forename: Xiqun
authors.initials: X
authors.lastname: Jiang
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000737:chemistry* / Q000633:toxicity; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry*; D006801:Humans; D053208:Kaplan-Meier Estimate; D051379:Mice; D008823:Micelles; D018613:Microscopy, Confocal; D009369:Neoplasms / Q000188:drug therapy / Q000401:mortality / Q000473:pathology; D011091:Polyesters / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*; D017550:Spectroscopy, Fourier Transform Infrared; D043823:Taxoids / Q000008:administration & dosage / Q000737:chemistry* / Q000633:toxicity; D014018:Tissue Distribution; D014183:Transplantation, Heterologous
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D008823:Micelles; D011091:Polyesters; D011108:Polymers; D043823:Taxoids; C016240:polycaprolactone; C552428:cabazitaxel