【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。更多还原

【Abstract】 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.更多还原