卟啉为核的星形聚己内酯-嵌段-聚乙二醇的合成及释放性能  

Synthesis and release property of porphyrin-cored star-shaped poly(ε-caprolactone)-block-poly(ethylene glycol)

作　　者：黄雅菲[1] 戈延茹[1] 戚雪勇[1] 戴晓晖[2] 

机构地区：[1]江苏大学药学院,江苏镇江212013 [2]江苏大学化学化工学院,江苏镇江212013

出　　处：《江苏大学学报（医学版）》2013年第3期247-253,共7页Journal of Jiangsu University：Medicine Edition

基　　金：国家自然科学基金资助项目(21004031);江苏省自然科学基金资助项目(BK2011459);江苏省博士后基金资助项目(1001034B)

摘　　要：目的:克服传统小分子卟啉药物的自淬灭,获得含卟啉药物核的靶向型高分子纳米微粒。方法:通过开环聚合和酯化反应合成了卟啉为核的聚己内酯-嵌段-聚乙二醇(SPPCL-b-PEO)共聚物,并利用凝胶渗透色谱、核磁共振谱、红外光谱、紫外可见光谱对其进行了表征。荧光探针法分析SPPCL-b-PEO的光动态效率。透射电镜观察SPPCL-b-PEO的自组装行为。紫外可见光谱分析SPPCL-b-PEO的载药及释放性能。结果:共聚物中大分子聚己内酯-聚乙二醇(PCL-PEO)骨架能有效延缓卟啉内核的自淬灭。随着共聚物中亲水聚己内酯(PCL)链段质量分数的减小,自组装胶束的形态由球状变为蠕虫状。负载多柔比星的SPPCL-b-PEO纳米微球具有较高的载药量和包封率,且体外释放具有pH依赖性。结论:潜在的卟啉核以及对pH 5～6的肿瘤组织靶向性使SPPCL-b-PEO满足抗肿瘤光动力治疗和肿瘤靶向给药系统的要求。Objective： In order to overcome the quenching of the traditional micromolecular porphyrin drug,the targeting polymer nanoparticles with porphyrin were obtained.Methods：Porphyrin-cored star-shaped poly（caprolactone）-block-poly（ethylene glycol） copolymers（SPPCL-b-PEO） were synthesized via ring-opening polymerization and esterification reaction,and were characterized by gel permeation chromatograph,nuclear magnetic resonance spectrum,fourier transform infrared spectroscopy and ultraviolet visible spectroscopy.The photosensitizing efficiency of SPPCL-b-PEO investigated by fluorescence probe method.The self-assembly behavior of SPPCL-b-PEO was investigated by transmission electron microscope.The drug loading and release properties of SPPCL-b-PEO were studied by ultraviolet visible spectroscopy.Results：The polymeric poly（caprolactone）-block-poly（ethylene glycol）（PCL-PEO） skeleton can efficiently prevent self-quenching of the central porphyrin in the copolymers.The self-assembled aggregates changed from spherical micelles to worm-like micelles with decreasing the weight fraction of hydrophilic poly（ethylene glycol）（PEO） block in the copolymers.The Doxorubicin-loaded SPPCL-b-PEO nanospheres possess the high drug content and entrapment efficiency,and exhibit property of pH-induced drug release.Conclusion： SPPCL-b-PEO will not only provide potential porphyrin core for photodynamic therapy but also improve targeting to pH5～6 tumor tissues for drug delivery.

关 键 词：开环聚合 酯化反应 卟啉 聚己内酯-聚乙二醇 多柔比星 

分 类 号：O636[理学—高分子化学]