嵌段共聚物聚乙二醇-聚苹果酸苄基酯载药胶束的制备及性质研究  

The Preparation of Methoxypolyethylene glycol-Poly(β-benzyl malate) of Loading-drug Micelle and Determination of Characteristics

作　　者：段晓[1] 李伟[1] 乔友备[1] 范黎[1] 吴红[1] 

机构地区：[1]第四军医大学药学院药物化学与药物分析教研室,陕西西安710032

出　　处：《现代生物医学进展》2013年第14期2625-2628,2621,共5页Progress in Modern Biomedicine

基　　金：国家自然科学基金项目(81271687;30970788)

摘　　要：目的:为构建聚合物胶束药物运载体系,制备嵌段共聚物聚乙二醇-聚苹果酸苄基酯载药胶束并测定其性质。方法:以L-天冬氨酸为原料,重氮化、环化后经开环聚合得到聚苹果酸苄基酯。氨基聚乙二醇通过酰胺键连接到β-聚苹果酸苄基酯上形成两亲性嵌段共聚物,喜树碱做药物模型制备载药胶束。动态光散射法测定胶束粒径、评价胶束稳定性,高效液相法测定喜树碱载药率和包封率,芘荧光法与动态光散射法测定临界胶束浓度。结果:喜树碱包封率72%,载药率6%,临界胶束浓度为40μg.mL-1。随着聚苹果酸苄基酯分子量减小,胶束稳定性增强。结论:聚乙二醇-聚苹果酸苄基酯在疏水链/亲水链分子量比值为2-4时在水中可自组装形成纳米胶束,可作为性能优良的聚合物药物载体。Objective： To prepare the methoxypolyethylene glycol-Poly（β-benzyl malate） loading-drug micelle,determine its characteristics and develop polymeric micelle drug delivery system.Methods： The synthesis of PMLABz was achieved via ring-opening polymerization from benzyl-β-malolactonate which achieved from L-aspartic acid thought diazotization reaction and cyclization reaction.Methoxypolyethylene glycol amine was covalently bound on Poly（β-benzyl malate）,then camptothecin was encapsulated to hydrophobic core.The particle size,entrapment efficiency,drug loading efficiency,critical micelle concentration and stability were measured by different techniques.Results： The camptothecin entrapment efficiency was 72 %,while drug loading efficiency was 6 %.The critical micelle concentration is 40 μg·mL-1,which is determined by pyrene fluorescence and dynamic light scattering.The smaller molecular weight of Poly-（β-benzyl malate） is,the more stable the micelles are.Conclusion： The micelle of methoxypolyethylene glycol-Poly（β-benzyl malate） co-polymer is a good drug carrier when hydrophobic/hydrophilic is 2-4.

关 键 词：聚苹果酸苄基酯 聚乙二醇 药物载体 胶束 

分 类 号：R944[医药卫生—药剂学]