摘要
目的制备冬凌草甲素单甲醚聚乙二醇-聚乳酸两亲性嵌段共聚物胶束,改善冬凌草甲素的水溶性。方法以单甲醚聚乙二醇-聚乳酸作为载体,采用丙酮溶剂挥发法和透析法制备不同药物/共聚物投料比的冬凌草甲素嵌段共聚物胶束。考察胶束相关性质。以载药量为评价标准,得出最佳投料比。结果电镜结果显示,胶束呈球形或类球形,载药量和包封率受制备方法和投料比的影响。透析法得到的胶束粒径较小,分散均匀度好,但载药量和包封率偏低。丙酮溶剂挥发法在药物共聚物的质量比例12.8:25.2时得到的胶束平均粒径为35.675 nm,载药量为22.1%,包封率为65.61%,粒径分布较窄,有利于纳米分散体系的稳定,且对冬凌草甲素有一定的增溶作用。结论聚乙二醇-聚乳酸嵌段共聚物胶束能够作为难溶性抗癌药物冬凌草甲素的良好纳米级载体。
Objective To prepare oridonin-loaded methxyl poly（ethylene glycol）-poly（lactic acid）（mPEG-PLA） block copolymer micelles for improving water solubility and bioavailability of oridonin. Methods The series mPEG-PLA block copolymer micelles with different drug/copolymer ratio were prepared by acetone solvent evaporation and dialysis methods.The optimal feed ratio was obtained on the basis of drug loaded. Results It was showed that micelles were sphericalunder transmission electron microscope（TEM）.Drug contents and loading efficiency of micelles affected the preparation and drug/copolymer ratio.Smaller particle size and better dispersion uniformity for micelles were gained by dialysis method,while the drug contents and loading efficiency were lower.The average particle size was 35.675 nm,the drug loading ratio was 22.1%,and loading efficiency ratio was 65.61% under the ratio of drug to copolymer as 12.8：25.2.The results reveal that the narrow particle distribution was benefit for the stability of dispersion system and improved water solubility. Conclusion The methxyl poly（ethylene glycol）-poly（lactic acid）block copolymer micelles could serve as good nanoscopic carriers for hydrophobic drug.
出处
《医药导报》
CAS
2010年第10期1334-1336,共3页
Herald of Medicine
