抗肿瘤药H6聚合物胶束的制备及体外抗肿瘤作用研究

发布时间：2018-05-01 22:12

本文选题：抗肿瘤药H + m　；参考：《中国药房》2017年04期

【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)(m PEG_(2000)-PCL_(4000))为载药材料,制备H6/m PEG_(2000)-PCL_(4000)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/m L、乙醇-氯仿为1∶1(V/V);所制备的H6/m PEG_(2000)-PCL_(4000)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IC_(50)分别为15.62、12.57 nmol/L,对H460细胞的IC_(50)分别为27.68、15.19 nmol/L。结论:成功制得H6/m PEG_(2000)-PCL_(4000)胶束,其具有体外抗肿瘤作用。
[Abstract]:Aim: to prepare anti-tumor drug H 6 (lactones) polymer micelles and to investigate its anti-tumor effect in vitro. Methods: using methoxy poly (ethylene glycol) (蔚 -caprolactone) as drug carrier, we prepared H6 / m PEGG / 2000- PCLL4 000 micelle. Particle size, polydispersity coefficient (PDI) and whether precipitation were produced at 48 h were used to screen the mass concentration of H6, the volume ratio of organic solvent and the entrapment efficiency and drug loading of the micelles. The toxicity of micelle and H6 solution to human non-small cell lung cancer cell line A549 and human lung cancer cell line H460 was detected by MTT assay. Results: the mass concentration of ethanol-chloroform was 1: 1 / 1 V / V / V / V = 1: 1 mg/m / L, and the particle size of H6 / m PEGG / P PEGG structure was 40.74 卤0.116 3nmPDI = 0.101 卤0.006, the entrapment efficiency was 94.87 卤0.016 ~ 3g / L, and the drug loading was 7.07 卤0.001 ~ 5ng / v / v ~ (-1) 路min ~ (-1) 路L ~ (-1) 路L ~ (-1) 路L ~ (-1) 路L ~ (-1) 路L ~ (-1) 路L ~ (-1) 路L ~ (-1) 路L ~ (-1). The ICs _ (50) of micelle and H _ 6 solution to A549 cells were 15.62 ~ 12.57 nmol / L, and to H460 cells were 27.68 ~ 15.19 nmol / L, respectively. Conclusion: h _ 6 / m PEGG _ (2 000) -PCL _ (4 000) micelle was successfully prepared, and it has antitumor effect in vitro.
【作者单位】：成都中医药大学药学院;四川大学生物治疗国家重点实验室;
【分类号】：R943;R96

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