阿霉素共聚物胶束的制备及体外性质研究

目的制备阿霉素共聚物胶束并研究其体外性质。方法采用开环聚合法合成聚乙二醇单甲醚-聚乳酸羟基乙酸（mPEG—PLGA）嵌段共聚物；用透析法、溶剂蒸发法制备空白及载阿霉素胶束；动态光散射仪（DLS）测定其粒径分布；采用紫外分光光度法测定胶束的包封率和载药量。通过体外释药实验研究了载阿霉素胶束的释药特性。结果采用透析法制备载阿霉素胶束大小均匀，平均粒径为（91．1±15．8）nm；药物胶束的包封率为85．2％，载药量为10．4％；与市售阿霉素注射剂相比，载阿霉素胶束具有良好的缓释性能。结论共聚物胶束可作为疏水性药物阿霉素的载体。

Preparation and Characterization of Doxorubicin-Loaded Block Copolymer Micelles in vitro

Objective To study preparation and properties of Doxorubicin-loaded-the po]y （D, L-lactic ae id-co- glycolide）-poly （ethyleneglycol） methoxy nano-micelles. Methods The poly （D, L-lactic ac id-co-glycolide ）-poly （ethyleneglycol） methoxy （abbreviated as mPEG-PLGA） was synthesized by ring-opening polymerization process,and the Doxorubicin（ DOX）-loaded micelles were prepared using the dialysis method and the solvent evaporation method. The dynamic light scattering was exploited to determine the particle size and the distribution of the micelles. The entrapment rate and drug-loading rate were determined by ultraviolet spectrophotometry. The release behavior of DOX from copolymer micelles was studied. Results The micelles had a mean diameter of （91.1 ± 15.8） nm prepared by the dialysis method. The entrapment rate was 85.2% and the drug loading of the micelles was 10.4%. DOX-loaded micelles have revealed long-circulation capability compare with DOX-injeetion. Conclusion The mPEG-/SLGA copolymer micelles may be applied as promising drug delivery system for DOX.