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抗肿瘤药H6聚合物胶束的制备及体外抗肿瘤作用研究
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| 篇名： | 抗肿瘤药H6聚合物胶束的制备及体外抗肿瘤作用研究 |
| TITLE： | |
| 摘要： | 目的：制备抗肿瘤药H6（内酯类化合物）聚合物胶束，考察其体外抗肿瘤作用。方法：以甲氧基聚乙二醇-聚（ε-己内酯）（mPEG2000-PCL4000）为载药材料，制备H6/mPEG2000-PCL4000胶束。以粒径、多分散系数（PDI）和48 h是否产生沉淀为指标筛选处方投料比、H6质量浓度、有机溶剂体积比，检测所制胶束的包封率和载药量。采用MTT法检测所制胶束与H6溶液对人非小细胞肺癌细胞A549、人肺癌细胞H460的毒性。结果：确定处方为投料比为1 ∶ 25、H6质量浓度为2 mg/mL、乙醇-氯仿为1 ∶ 1（V/V）；所制备的H6/mPEG2000-PCL4000胶束的粒径为（40.74±0.116 3） nm，PDI为0.101±0.006，包封率为（94.87±0.016 3）％，载药量为（7.07± 0.001 5）％（n＝3）。胶束和H6溶液对A549细胞的IC50分别为15.62、12.57 nmol/L，对H460细胞的IC50分别为27.68、15.19 nmol/L。结论：成功制得H6/mPEG2000-PCL4000胶束，其具有体外抗肿瘤作用。 |
| ABSTRACT： | OBJECTIVE： To prepare anti-tumor drug H6 （lactone compound） polymeric micelles， and to investigate its in vitro anti-tumor effects. METHODS： Using mPEG2000-PCL4000 as carrier， H6/mPEG2000-PCL4000 micelles were prepared. Using particle size， PDI and 48 h whether to produce precipitation as indexes， feeding ratio， H6 concentration， volume ratio of organic solvent were screened. The encapsulation efficiency and drug-loading amount of micelle were all detected. MTT assay was used to detect the toxicity of micelles and H6 solution to human non-small cell lung cancer cell A549 and human lung cancer cell H460. RESULTS： The screened formulation was as follows as feeding ratio of 1 ∶ 25， H6 concentration of 2 mg/mL， the ratio of ethanol to chloroform of 1 ∶ 1 （V/V）. The parameters of prepared H6/mPEG2000-PCL4000 micelles were as follows as particle size of （40.74±0.116 3） nm， PDI of （0.101±0.006）， encapsulation efficiency of （94.87±0.016 3）％， drug-loading amount of （7.07±0.001 5）％ （n＝3）. IC50 of micelles and H6 solution to A549 cell were 15.62 and 12.57 nmol/L； IC50 of micelles and H6 solution to H460 cell were 27.68 and 15.19 nmol/L. CONCLUSIONS： H6/mPEG2000-PCL4000 micelles are prepared successfully and show in vitro anti-tumor effects. |
| 期刊： | 2017年第28卷第4期 |
| 作者： | 潘超，刘会丽，许俊鹏，唐俏欣，万丽 |
| AUTHORS： | PAN Chao，LIU Huili，XU Junpeng，TANG Qiaoxin，WAN Li |
| 关键字： | 抗肿瘤药H6；mPEG2000-PCL4000；胶束；抗肿瘤作用 |
| KEYWORDS： | Anti-tumor drug H6； mPEG2000-PCL4000； Micelles； Anti-tumor effect |
| 阅读数： | 404 次 |
| 本月下载数： | 4 次 |
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