胶束
共聚物
动态光散射
乙二醇
分散性
Zeta电位
两亲性
共轭体系
化学
高分子化学
材料科学
水溶液
纳米颗粒
有机化学
纳米技术
聚合物
作者
Cinzia Garofalo,G. A. Capuano,Rosa Sottile,Rossana Tallerico,Renata Adami,Ernesto Reverchon,Ennio Carbone,Lorella Izzo,Daniela Pappalardo
出处
期刊:Biomacromolecules
[American Chemical Society]
日期:2013-12-23
卷期号:15 (1): 403-415
被引量:76
摘要
One constrain in the use of micellar carriers as drug delivery systems (DDSs) is their low stability in aqueous solution. In this study “tree-shaped” copolymers of general formula mPEG-(PLA)n (n = 1, 2 or 4; mPEG = poly(ethylene glycol) monomethylether 2K or 5K Da; PLA = atactic or isotactic poly(lactide)) were synthesized to evaluate the architecture and chemical composition effect on the micelles formation and stability. Copolymers with mPEG/PLA ratio of about 1:1 wt/wt were obtained using a “core-first” synthetic route. Dynamic Light Scattering (DLS), Field Emission Scanning Electron Microscopy (FESEM), and Zeta Potential measurements showed that mPEG2K-(PD,LLA)2 copolymer, characterized by mPEG chain of 2000 Da and two blocks of atactic PLA, was able to form monodisperse and stable micelles. To analyze the interaction among micelles and tumor cells, FITC conjugated mPEG-(PLA)n were synthesized. The derived micelles were tested on two, histological different, tumor cell lines: HEK293t and HeLa cells. Fluorescence Activated Cells Sorter (FACS) analysis showed that the FITC conjugated mPEG2K-(PD,LLA)2 copolymer stain tumor cells with high efficiency. Our data demonstrate that both PEG size and PLA structure control the biological interaction between the micelles and biological systems. Moreover, using confocal microscopy analysis, the staining of tumor cells obtained after incubation with mPEG2K-(PD,LLA)2 was shown to be localized inside the tumor cells. Indeed, the mPEG2K-(PD,LLA)2 paclitaxel-loaded micelles mediate a potent antitumor cytotoxicity effect.
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