叶酸受体靶向的聚乳酸共聚物胶束的制备及性质研究

Preparation of folate receptor targeted micelles from polylactic acid copolymers and study on their properties

叶酸偶联的羟脯氨酸-乳酸共聚物(PLLA-PHpr-FA)是一种新型的叶酸受体靶向生物降解聚合物,研究PLLA-PHpr-FA自组装形成胶束的能力及胶束的性质。临界胶束浓度(CMC)用芘荧光探针测定,结果表明,CMC很低并依赖于乳酸/羟脯氨酸的比例。透射电子显微镜(TEM)显示共聚物胶束呈现典型的核/壳结构。动态激光光散射(DLS)测定粒径及粒径分布结果显示,粒径受乳酸/羟脯氨酸比例和丙酮量调控,但粒子几乎不受稀释的影响。用紫外分光光度法测定胶束的载药量和包封率表明,共聚物胶束对疏水性药物的包载较好。因此,PLLA-PHpr-FA胶束可以作为肿瘤靶向的药物载体。

The copolymer of L-lactide and 4-hydroxyproline with folate（PLLA-PHpr-FA） is a new kind of folate receptor targeted polylactic acid copolymers.This article aimed to research the self-assembly micelles and the properties of the micelles prepared from PLLA-PHpr-FA.The critical micelle concentration（CMC） was determined with fluorescent probe method,the results showed that the CMCs were quite low and dependent on the molar ratio of lactide/HP.Transmission electron microscope（TEM） indicated that the micelles presented typical core/shell structure.Dynamic light scattering（DLS） was used to measure the particle size and particle size distribution.The size of the particles was found to be regulated by the lactide/HP ratio and the amount of the acetone,but nanoparticle aqueous solution hardly changed over the dilution.The drug contents and loading efficiency of the micelles were investigated with UV spectrophotometry.The result showed that loading efficiency of the micelles for hydrophobic drug was good.Therefore,PLLA-PHpr-FA micelles might serve as a novel potential carrier targeted tumors for drug delivery.