紫杉烷衍生物/PEG-PLA胶束的制备及理化性质研究  

Preparation and characterization of taxane derivative TM-2 polymer micelles

作　　者：王俏 刘懿 唐星[1] 王艳娇[1] WANG Qiao;LIU Yi;TANG Xing;WANG Yanjiao(School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China)

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2019年第10期869-873,共5页Journal of Shenyang Pharmaceutical University

摘　　要：目的采用两亲性聚合物材料聚乙二醇-聚乳酸(PEG-PLA)为载体,紫杉烷衍生物TM-2作为模型药物,制备出高载药量的胶束制剂。方法采用凝胶渗透色谱法、差示扫描量热法、核磁、红外等方法对聚合物材料性质进行表征,芘荧光探针法测定材料的临界胶束浓度,通过薄膜水化法制备聚合物胶束,并对胶束溶液进行冻干,考察胶束的粒径、电位、载药量、体外释放等理化性质。结果胶束粒径约为20 nm,载药量在10%左右,冻干后体外释放可在72 h内释放80%以上。结论以无定型形式存在的TM-2通过薄膜水化法与聚合物自组装增加其在水中的溶解度,体外释放起始可能是因附在粒子表面或近表面的药物快速释放,随后通过载体孔道扩散而缓慢释放。Objective To prepare high-loading micelle preparations using amphiphilic polymer materials as carrier and taxane derivative TM-2 as a model drug.Methods The properties of polymer materials were characterized by gel permeation chromatography,differential scanning calorimetry,nuclear magnetic resonance and infrared spectroscopy.The critical micelle concentration of the material was determined by fluorescence probe method.The polymer gel was prepared by the thin-film hydration method.In order to increase the stability of micelles,the micelles were lyophilized.The micellar appearance,particle size,potential,drug loading,and in vitro release were investigated in this study.Results TM-2 polymer micelles prepared by thin-film hydration method increased the solubility of the drug in water.The appearance of the micelles was good before and after freeze-drying.The particle size was 30 nm and the drug loading was 10%.And the in vitro release of micelles after freeze-drying could release 80%in 72 h.Conclusion TM-2 in its amorphous form increased its solubility in water by self-assembly.In vitro release may be due to the rapid release of drug attached to or near the surface of the particle,followed by diffusion through the pores of the carrier.

关 键 词：TM-2 聚合物胶束 薄膜水化法 高载药量 体外释放 

分 类 号：R943[医药卫生—药剂学]