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表柔比星聚乳酸-羟基乙酸共聚物微球的制备及抗肿瘤活性研究
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| 篇名： | 表柔比星聚乳酸-羟基乙酸共聚物微球的制备及抗肿瘤活性研究 |
| TITLE： | |
| 摘要： | 目的：制备表柔比星聚乳酸-羟基乙酸共聚物（PLGA）微球，并考察其体外抗肿瘤活性。方法：以PLGA为载体，采用乳化-溶剂挥发法制备表柔比星PLGA微球。利用透射电子显微镜观察微球的形态结构，激光粒度分布测量仪检测其粒径分布；紫外分光光度法测定其主药含量，计算载药量和包封率；通过体外释放试验考察10 d内的累积释放度；采用MTT法检测所制微球和表柔比星对人乳腺癌MCF-7细胞的增殖抑制率。结果：所制表柔比星PLGA微球的粒径为（175.2±16.8） μm，载药量为（8.6±1.3）％，包封率为（46.7±8.6）％（n＝7）；4 h、24 h、10 d累积释放度分别为27.8％、41.7％、92.3％。与表柔比星比较，表柔比星PLGA微球能延长对人乳腺癌MCF-7细胞的增殖抑制率至96 h（表柔比星48 h的抑制率为96.7％，表柔比星PLGA微球96 h的抑制率为99.3％）。结论：成功制得表柔比星PLGA微球，其具有良好的体外缓释效果和抗肿瘤活性。 |
| ABSTRACT： | OBJECTIVE： To prepare epirubicin-loaded PLGA microspheres and study its in vitro antitumor activity. METHODS： Using PLGA as carrier， epirubicin-loaded PLGA microspheres were prepared by using emulsification-solvent evaporation method. The morphology of microspheres was observed by TEM； the distribution of particle size was determined by laser granularity distribution measuring instrument； the content of main component was determined by UV spectrophotometry. The drug-loading amount and entrapment efficiency were calculated， and accumulative release rate （Q） was investigated by in vitro release test within 10 d. The proliferation inhibitory rates of prepared microspheres and epirubicin to human breast cancer MCF-7 cells were detected by MTT assay. RESULTS： The particle size， drug-loading amount and encapsulation efficiency of epirubicin-loaded PLGA microspheres were （175.2±16.8） μm， （8.6±1.3）％ and （46.7±8.6）％（n＝7）； Q4 h， Q24 h and Q10 d were 27.8％， 41.7％ and 92.3％， respectively. Compared with epirubicin， epirubicin-loaded PLGA microspheres could prolong inhibitory rate of epirubicin to MCF-7 cells for 96 h （48 h inhibitory rate of epirubicin was 96.7％， 96 h proliferation inhibitory rate of Epirubicin-loaded PLGA microspheres was 99.3％）. CONCLUSIONS： Epirubicin-loaded PLGA microspheres are prepared successfully， and show good in vitro sustained-release effect and antitumor activity. |
| 期刊： | 2016年第27卷第34期 |
| 作者： | 刘炜，王晓彤，刘菊 |
| AUTHORS： | LIU Wei，WANG Xiaotong，LIU Ju |
| 关键字： | 表柔比星；聚乳酸-羟基乙酸共聚物；微球；抗肿瘤活性 |
| KEYWORDS： | Epirubicin； PLGA； Microspheres； Antitumor activity |
| 阅读数： | 326 次 |
| 本月下载数： | 6 次 |
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