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以pH敏感型两亲性嵌段共聚物聚乙二醇-聚(2,4,6-三甲氧基苯甲缩醛季戊四醇碳酸酯)为载体,采用透析法制备了多柔比星胶束,并表征了胶束的理化性质。所得载药胶束呈球形且分布均匀,平均粒径为(163.3±2.1)nm,电位为(-17.54±0.26)mV,载药量为10.3%,包封率为68.9%。不同pH值介质对载药胶束的粒径和体外释放行为有显著影响。在pH 5.0介质中胶束粒径会在24 h内明显增大至800~1 000 nm,且2 h时有明显突释,48 h累积释放率达90%。体外毒性试验表明,空白胶束对正常和肿瘤细胞均没有明显毒性,载药胶束对B16黑素瘤细胞具有明显毒性,且呈浓度依赖性。
A pH-sensitive amphiphilic block copolymer polyethylene glycol-poly (2,4,6-trimethoxybenzaldehyde pentaerythritol carbonate) was used as a carrier to prepare doxorubicin micelles by dialysis method. And characterize the physicochemical properties of micelles. The drug-loaded micelles were spherical and evenly distributed. The average particle diameter was (163.3 ± 2.1) nm, and the potential was (-17.54 ± 0.26) mV. The drug loading was 10.3% and the entrapment efficiency was 68.9%. Different pH media have significant effect on particle size and in vitro release of drug-loaded micelles. At pH 5.0, the size of micelles increased significantly from 800 to 1 000 nm in 24 h, with a pronounced burst at 2 h and a cumulative release rate of 90% at 48 h. In vitro toxicity tests showed that the blank micelles had no obvious toxicity on normal and tumor cells, and drug-loaded micelles were obviously toxic to B16 melanoma cells in a concentration-dependent manner.