Nanoparticles with typical core-shell structure were prepared with a blend of methoxypoly（ethylene glycol）-poly（lactide） copolymer （MPEG-PLA） and poly （lactic acid） （PLA） along with paclitaxel by the O/W sol...Nanoparticles with typical core-shell structure were prepared with a blend of methoxypoly（ethylene glycol）-poly（lactide） copolymer （MPEG-PLA） and poly （lactic acid） （PLA） along with paclitaxel by the O/W solvent evaporation method. An orthogonal experiment L9（3）3 was applied to get the best preparation conditions. The core-shell paclitaxel-loaded MPEG-PLA/PLA nanoparticles with the highest drug loading efficiency were obtained when amount of MPEG-PLA, time of ultrasonication and volume of deionized water were 300 mg, 10 rain and 30 mL, respectively. The release behavior of paclitaxel from the optimal MPEG-PLA/PLA nanoparticles showed that 22% ofpaclitaxel was released in 14 d. When incubating with human nasopharyngeal carcinoma ceils expressing LMP 1, these optimal nanoparticles showed a little lower tumor growth compared with free paclitaxel.展开更多
基金Key Research Foundation of Wannan Medical College(Grant No.WK2014Z06)Doctoral Starting-up Foundation of Wannan Medical College(Grant No.201219)
文摘Nanoparticles with typical core-shell structure were prepared with a blend of methoxypoly（ethylene glycol）-poly（lactide） copolymer （MPEG-PLA） and poly （lactic acid） （PLA） along with paclitaxel by the O/W solvent evaporation method. An orthogonal experiment L9（3）3 was applied to get the best preparation conditions. The core-shell paclitaxel-loaded MPEG-PLA/PLA nanoparticles with the highest drug loading efficiency were obtained when amount of MPEG-PLA, time of ultrasonication and volume of deionized water were 300 mg, 10 rain and 30 mL, respectively. The release behavior of paclitaxel from the optimal MPEG-PLA/PLA nanoparticles showed that 22% ofpaclitaxel was released in 14 d. When incubating with human nasopharyngeal carcinoma ceils expressing LMP 1, these optimal nanoparticles showed a little lower tumor growth compared with free paclitaxel.
文摘本文以可降解聚合物单甲氧基聚乙二醇-聚乳酸聚乙醇酸(Me PEG-PLGA)为载体,羟基喜树碱(HCPT)为模型药物,利用SPG(Shirasu porous glass membrane)模板法,通过正交设计优化制备了彗星状MePEG-PLGA-HCPT共聚物粒子。采用动态光散射分析、扫描/透射电镜、X-射线衍射法和差示扫描量热法等研究载药粒子的粒径、zeta电位、载药量、收率、形态和HCPT的存在状态;初步评价了载药粒子的体外释药;MTT法初步考察对肝癌BEL-7402细胞的毒性作用。结果显示,最佳制备条件为:HCPT与MePEG-PLGA的质量比为1∶1,氮气压力为100 k Pa,SPG膜孔径为1.1μm;载药粒子在电镜下呈彗星状,其中头部螺旋成束,尾部为散开的纳米束;粒子的载药量可达到46.2%,收率为96.4%,zeta电位为-31.4 m V;HCPT以无定形态均匀分布于MePEG-PLGA粒子中,具有药物缓释的优点,且药物释放的速度随着载药量的增加而增大;该形貌的载药粒子相对于球形载药粒子对肝癌BEL-7402细胞的抑制作用更强,有用于肿瘤临床治疗的潜能。
