紫杉醇溫敏脂質(zhì)體與siRNA金納米星載藥系統(tǒng)的構(gòu)建與表征
發(fā)布時(shí)間:2018-04-28 21:09
本文選題:紫杉醇 + 溫敏脂質(zhì)體; 參考:《中國(guó)藥科大學(xué)學(xué)報(bào)》2017年04期
【摘要】:用種子生長(zhǎng)法制備金納米星(gold nanostar,GNS),構(gòu)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)修飾的載COX-2 siRNA(siCOX-2)的GNS復(fù)合納米粒[siCOX-2(9R/DG-GNS)];以薄膜分散法制備載紫杉醇溫敏脂質(zhì)體(paclitaxel temperature sensitive liposome,PTX-TSL);最后將siCOX-2(9R/DG-GNS)與PTX-TSL體通過(guò)巰基配位得到PTX-TSL與siCOX-2(9R/DG-GNS)共載藥系統(tǒng)PTX-TSL-[siCOX-2(9R/DG-GNS)]。采用核磁共振、聚丙烯酰胺凝膠電泳、紫外分光光度法、瓊脂糖凝膠電泳法驗(yàn)證了siCOX-2(9R/DG-GNS)成功構(gòu)建,馬爾文電位粒度儀測(cè)得PTX-TSL-[siCOX-2(9R/DG-GNS)]粒徑電位分別為(292±14)nm、-(2.59±0.12)m V,透射電子顯微鏡結(jié)果顯示其結(jié)構(gòu)呈包裹磷脂雙分子層的星型,808 nm激光照射下表現(xiàn)出良好的光熱轉(zhuǎn)換效率。差示掃描量熱法測(cè)試PTX-TSL相變溫度約為42.6℃,透析法測(cè)得其載藥量為7.5%,包封率為95.4%,具有良好的溫敏釋藥性能。因此,本復(fù)合物納米載藥系統(tǒng)可作為PTX與siCOX-2的共載藥體系,用以抗腫瘤耐藥治療。
[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 鹵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 鹵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,
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