多柔比星聚合物胶束制备、表征及其体外释药研究

发布时间：2018-03-30 21:48

本文选题：多柔比星　切入点：Soluplus　出处：《中国抗生素杂志》2015年07期

【摘要】：目的制备多柔比星的soluplus聚合物胶束,并对其进行体外评价。方法采用薄膜分散法-p H诱导法相结合制备多柔比星聚合物胶束;采用粒径测定仪、透射电镜、X-射线衍射(XRD)、差示扫描量热法(DSC)及红外光谱(FTIR)对其进行表征;采用HPLC法测定胶束的包封率和载药量;采用动态膜透析法考察载药胶束的体外释药特性。结果本研究制备的胶束呈球形或类球形,平均粒径为(67.57±2.9)nm,平均包封率为(77.81±4.03)%,平均载药量(10.15±1.56)%;XRD和DSC结果表明多柔比星以无定型状态或分子状态包载在聚合物胶束中;FTIR结果表明多柔比星分子中羟基和聚合物的羰基之间形成了氢键;体外释放结果表明多柔比星的soluplus聚合物胶束具有缓释作用。结论该胶束制备工艺简单,其粒径、包封率、载药量可控,具有缓释作用。
[Abstract]:Objective to prepare soluplus polymer micelles of doxorubicin and evaluate it in vitro. It was characterized by transmission electron microscopy (TEM), X-ray diffraction (XRD), differential scanning calorimetry (DSC) and infrared spectroscopy (FTIR), and the encapsulation efficiency and drug loading of micelles were determined by HPLC method. The release characteristics of drug-loaded micelles in vitro were investigated by dynamic membrane dialysis. Results the micelles prepared in this study were spherical or spherical. The average particle size was 67.57 卤2.9 nm, the average entrapment efficiency was 77.81 卤4.03, and the average drug loading was 10.15 卤1.56 nm. The results of DSC and XRD showed that doxorubicin was carried in amorphous state or molecular state package in the polymer micelle. The results of FTIR showed that doxorubicin was hydroxyl and carbonyl group of polymer in doxorubicin molecule. Hydrogen bonds formed between them; The results of in vitro release showed that the soluplus polymer micelles of doxorubicin had a sustained release effect. Conclusion this micelle has a simple preparation process, its particle size, entrapment efficiency, drug loading is controllable, and it has a sustained release effect.
【作者单位】：广东医学院药学院;
【基金】：广东省科技计划项目(No.2014A020212296) 东莞市国际合作项目(No.2013508152013) 广东省青年创新项目(2014) 广东省大学生创新项目(No.1057113028,1057112043)
【分类号】：R943

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