紫杉醇温敏脂质体与siRNA金纳米星载药系统的构建与表征

发布时间：2018-04-28 21:09

  本文选题：紫杉醇 + 温敏脂质体　； 参考：《中国药科大学学报》2017年04期

【摘要】：用种子生长法制备金纳米星(gold nanostar,GNS),构建聚乙二醇(polyethylene glycol,PEG)、氨基葡萄糖(2-amino-2-deoxy-D-glucose,DG)和九聚精氨酸(9-D-arginine,9R)修饰的载COX-2 siRNA(siCOX-2)的GNS复合纳米粒[siCOX-2(9R/DG-GNS)];以薄膜分散法制备载紫杉醇温敏脂质体(paclitaxel temperature sensitive liposome,PTX-TSL);最后将siCOX-2(9R/DG-GNS)与PTX-TSL体通过巯基配位得到PTX-TSL与siCOX-2(9R/DG-GNS)共载药系统PTX-TSL-[siCOX-2(9R/DG-GNS)]。采用核磁共振、聚丙烯酰胺凝胶电泳、紫外分光光度法、琼脂糖凝胶电泳法验证了siCOX-2(9R/DG-GNS)成功构建,马尔文电位粒度仪测得PTX-TSL-[siCOX-2(9R/DG-GNS)]粒径电位分别为(292±14)nm、-(2.59±0.12)m V,透射电子显微镜结果显示其结构呈包裹磷脂双分子层的星型,808 nm激光照射下表现出良好的光热转换效率。差示扫描量热法测试PTX-TSL相变温度约为42.6℃,透析法测得其载药量为7.5%,包封率为95.4%,具有良好的温敏释药性能。因此,本复合物纳米载药系统可作为PTX与siCOX-2的共载药体系,用以抗肿瘤耐药治疗。
[Abstract]:COX-2 siRNAsiCOX-2 GNS nanoparticles modified by PEGG, 2-amino-2-deoxy-D-glucose (2-amino-2-deoxy-D-glucose) and 9-arginine (9-D-arginine 9R) were prepared by seed growth method. The GNS nanoparticles (siCOX-2pac-9RDG-GNG-GNS) were prepared by thin-film dispersion, and the thermo-sensitive paclitaxel temperature sensitive liposome PTX-TSLs were prepared by thin-film dispersion method. Finally, the co-loaded drug system PTX-TSL- [SiCOX-2R- 9R / DG-GNS-] was obtained by mercapto coordination of siCOX-2R / DG-GNS with PTX-TSL. Nuclear magnetic resonance (NMR), polyacrylamide gel electrophoresis (PAGE), ultraviolet spectrophotometry (UV) and agarose gel electrophoresis (agarose) were used to verify the successful construction of siCOX-2X 9R / DG-GNS. The particle size potential of PTX-TSL- [SiCOX-2O9R / DG-GNS] was 2.59 卤0.12mV, respectively. The results of transmission electron microscopy showed that the PTX-TSL- [siox-2r-9R / DG-GNS] particle size potential was 2.59 卤0.12mV, respectively. The results of transmission electron microscopy showed that the PTX-TSL- [SiCOX-2O9R- DG-GNSs] exhibited a good photothermal conversion efficiency under the irradiation of a star type 808nm laser. The phase change temperature of PTX-TSL measured by differential scanning calorimetry is about 42.6 鈩，

本文编号：1816879