两亲性聚合物聚乙二醇单甲醚-聚乳酸-β-环糊精的合成、表征及载药性能

Synthesis,characterization and properties as a drug carrier of the amphiphilic MPEG-PLA-β-CD

以丁二酸酐为连接臂,将不同相对分子质量的聚乙二醇单甲醚-聚乳酸(MPEG-PLA)分别连接到N-(2-氨乙基)胺基-β-环糊精上,制备得4个未见文献报道的不同相对分子质量的两亲性聚乙二醇单甲醚-聚乳酸-β-环糊精(MPEG-PLA-β-CD)。采用FT-IR与1H NMR对其结构进行表征,采用芘荧光探针光谱法测定其临界胶束浓度(critical micelle con-centration,CMC)。并以布洛芬为模型药物初步考察4个聚合物的载药性能。其中MPEG 2K-PLA 6.6K-β-CD具有较小的CMC和较高的载药能力,有望成为良好的药物载体材料。

A novel series of amphiphilic polymers,MPEG-PLA-β-CD,with different relative molecular weight were synthesized by conjugating MPEG-PLA onto 6-deoxy-6-ethylenediamino-β-cyclodextrin through succinic anhydride as spacers.The chemical structures were characterized by FT-IR and 1H NMR.The critical micelle concentrations（CMCs） were determined by pyrene fluorescence probe spectrometry.These polymers could self-assemble into micelles loading hydrophobic drugs.Diameters,the drug-encapsulation efficiency and drug-loading efficiency of the micelles loading ibuprofen were also measured to investigate the properties of polymers as drug delivery systems.According to the results,MPEG 2K-PLA 6.6K-β-CD was a potential drug delivery agent owing to its lower CMC value and higher drug-loading efficiency.