摘要
目的:制备多西紫杉醇的聚合物胶束,提高其在水中的溶解度。方法:用开环反应合成不同比例的聚乳酸-聚乙二醇单甲醚(PLA-mPEG)共聚物,通过DSC、IR、1HNMR确证其结构,荧光法测定其临界胶束浓度(CMC)。以溶剂蒸发-固体熔融分散法制备多西紫杉醇聚合物胶束,正交设计优化其制备工艺。HPLC测定其载药量、包封率,激光粒度仪测定其粒径及分布,IR确证含药胶束的形成。结果:采用比例为6/4的PLA-mPEG共聚物为载体,以乙腈为有机溶剂制备,所得胶束平均粒径为47.0nm,载药量为27.3%,包封率为97.4%,且IR确证药物已被包封在胶束中,而非物理混合。结论:PLA-mPEG聚合物胶束能显著提高多西紫杉醇在水中的溶解度。
Aim： To synthesize poly （ D, L-lactic acid） -poly （ ethylene glycol） methoxy （PLA-mPEG） block polymer and prepare PLA-mPEG polymer micelles in order to improve the solubility of docetaxel in water. Methods： Poly （D, L-lactic acid）-poly （ethylene glycol） methoxy （PLA-mPEG） block polymer was synthesized by ring opening reaction in different proportionality of D, L-lactide and mPEG and their structures were identified by DSC, IR, ^1H NMR. The values of CMC were determinated by fluorometric method. The polymer micelles containing docetaxel were prepared by solvent evaporation-solid melting method. The optimization preparation condition was gained by orthogonal experimental design. The drug loading encapsulation were determined by HPLC. The mean diameter and distribution of the particle size were also assayed. The formulation of drug-loading micelles was confirmed by IR. Results： The preparation condition of the micelles is that the polymer with the proportion of 6/4 as carrier, acetonitrile as organic solvent. The mean diameter was 47.0 nm, and drug loading as well as the encapsulation efficiency were 27.3% and 97.4%, respectively. Docetaxel was found to be encapsulated in the micelles rather exist a physical mixture. Conclusion： Docetaxel PLA-mPEG polymer micelles can obviously improves the solubility of docetaxel.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2008年第3期223-227,共5页
Journal of China Pharmaceutical University
