载阿霉素PLGA-PLL-PEG纳米粒的制备及抑瘤作用研究
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篇名: 载阿霉素PLGA-PLL-PEG纳米粒的制备及抑瘤作用研究
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摘要: 目的:制备载阿霉素聚乳酸羟基乙酸-聚赖氨酸-聚乙二醇(PLGA-PLL-PEG)纳米粒,并研究其抑瘤作用。方法:应用PLGA-PLL和活化PEG聚合而成的PLGA-PLL-PEG为载体包载阿霉素,制得载阿霉素PLGA-PLL-PEG纳米粒。检测纳米粒的形态大小、粒径分布、阿霉素的含量,计算载药量和包封率,比较纳米粒和阿霉素在144 h内的累积释放率(Q)和对乳腺癌HeLa细胞的增殖抑制率,计算半数抑制率(IC50)。结果:所制载阿霉素PLGA-PLL-PEG纳米粒为规则圆形,分散性良好,无黏连,平均粒径为(136.7±9.3) nm(n=5),平均包封率为(76.67±8.63)%,平均载药量为(3.86±0.55)%(n=3);阿霉素的Q12 h达100%,载阿霉素PLGA-PLL-PEG纳米粒的Q24 h为52.9%、Q144 h为81.2%。载阿霉素PLGA-PLL-PEG纳米粒对HeLa细胞的增殖抑制率较阿霉素增长缓慢,二者的IC50分别为1.844、0.345 μg/mL。结论:成功制得载阿霉素PLGA-PLL-PEG纳米粒,其具有良好的缓释效果,其抑瘤作用强于阿霉素。
ABSTRACT: OBJECTIVE: To prepare adriamycin-loaded PLGA-PLL-PEG nanoparticles, and study its antitumor activity. METHODS: PLGA-PLL-PEG with the polymerization of PLGA-PLL and activated polyethylene glycol was used as carrier for adriamycin, and adriamycin-loaded PLGA-PLL-PEG nanoparticles were prepared. The shape size, particle size distribution, adriamycin content of nanoparticles were detected, drug loading and encapsulation efficiency were calculated. Cumulative release rate (Q) of nanoparticles and adriamycin within 144 h and its proliferation inhibition rate on breast cancer HeLa cells were compared, and half inhibitory rate (IC50) was calculated. RESULTS: Prepared adriamycin-loaded PLGA-PLL-PEG nanoparticles were regular circular with good dispersion and no adhesion. The average particle size was (136.7±9.3) nm (n=5), average encapsulation efficiency was (76.67±8.63)%, average drug loading was (3.86±0.55)% (n=3). Q12 h of adriamycin had reached 100%; Q12 h of adriamycin-loaded PLGA-PLL-PEG nanoparticles was 52.9%, Q144 h was 81.2%. The inhibitory rate of adriamycin-loaded PLGA-PLL-PEG nanoparticles on HeLa cells increased slowly than adriamycin; IC50 were 1.844, 0.345 μg/mL, respectively. CONCLUSIONS: Adriamycin-loaded PLGA-PLL-PEG nanoparticles are prepared successfully, showing good sustained-release effect and more significant inhibitory effect than adriamycin.
期刊: 2017年第28卷第16期
作者: 刘炜,王晓彤,王建华
AUTHORS: LIU Wei,WANG Xiaotong,WANG Jianhua
关键字: 阿霉素;聚乳酸羟基乙酸-聚赖氨酸;聚乙二醇;纳米粒;肿瘤细胞;抑制
KEYWORDS: Adriamycin; PLGA-PLL; PEG; Nanoparticles; Tumor cells; Inhibitory
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