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紫杉醇温敏脂质体与siRNA金纳米星载药系统的构建与表征
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引用本文:程紫婷,姚珂,刘婉婉,许伯慧,朱红艳.紫杉醇温敏脂质体与siRNA金纳米星载药系统的构建与表征[J].中国药科大学学报(中文版),2017,48(4):445-452
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作者单位
程紫婷 南通大学药学院 
姚珂 南通大学药学院 
刘婉婉 南通大学药学院 
许伯慧 南通大学药学院 
朱红艳 南通大学药学院 
基金项目:国家自然科学基金资助项目(No.81202467);江苏省自然科学基金资助项目(No.BK2012232);南通大学大学生创新训练计划项目(No.2016129)
中文摘要: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)mV,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。
中文关键词:紫杉醇  温敏脂质体  氨基葡萄糖  金纳米星  siCOX-2
 
Preparation and characterization of composite delivery system of paclitaxel-loaded temperature sensitive liposome and siRNA-loaded gold nanostar
Abstract:We prepared gold nanostar(GNS)through seed growth method firstly, then formation of COX-2 siRNA(siCOX-2)and GNS composite modified with polyethylene glyco(PEG), 2-amino-2-deoxy-D-glucos(DG)and 9-D-arginin(9R)was prepared. Afterwords, paclitaxel temperature sensitive liposome(PTX-TSL)was prepared by film dispersion method. Finally, siCOX-2 delivery systerm(PTX-TSL-(siCOX-2(9R/DG-GNS)))was obtained by hydrosulfuryl ligand reaction between siCOX-2(9R/DG-GNS)and PTX-TSL. The successful build of siCOX-2(9R/DG-GNS)was vetified by nuclear magnetic resonance(NMR), sodium dodecyl sulfate polyacryl amide gel electrophoresis(SDS-PAGE), and ultraviolet spectrophotometry and agarose gel electrophoresis method. Particle size of PTX-TSL-(siCOX-2(9R/DG-GNS))was(292±14)nm and Zeta potential was about -(2. 59±0. 12)mV, which were measured by Zetasizer Nano ZS90. The morphology of PTX-TSL-(siCOX-2(9R/DG-GNS))measured by transmissionelectronmicroscopy showed homogeneous star structure with phospholipid bilayer on the surface, and it showed good thermal conversion efficiency under radiation of 808 nm laser. Differential scanning calorimetry test showed that PTX-TSL phase transition temperature is about 42. 6 °C. The drug loading content(using dialysis method)and encapsulation efficiency of PTX-TSL were about 7. 5% and 95. 4%, at the same time, the release process experiment of PTX-TSL showed that it had a good temperature sensitive release performance. It is hopeful that this siCOX-2 system can be used for reducing drug resistance of PTX and improving the treatment effect of PTX through the synergistic antitumor drug resistance effect of siCOX-2.
keywords:paclitaxel  temperature sensitive liposome  2-amino-2-deoxy-D-glucos  gold nanostar  siCOX-2
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