米托蒽醌隐形阳离子脂质体的制备及体内外抗肿瘤活性

发布时间：2018-07-14 15:30

【摘要】：目的:制备米托蒽醌隐形阳离子脂质体(YM),并研究其制剂学性质及体内外抗肿瘤作用。方法:膜材料中引入2-二油酰基羟丙基-3-N,N,N-三甲铵氯(DOTAP)和聚乙二醇2000-二硬脂酰磷脂乙醇胺(DSPE-PEG2000)分别作为阳性和隐形膜材,采用硫酸铵梯度法制备YM,并以泄漏率为指标,考察其稳定性;高内涵扫描仪考察2 h时其在B16F10细胞中的摄取情况;MTT法测定其对B16F10细胞的增殖影响;B16F10皮下移植瘤模型研究其体内抗肿瘤作用。结果:YM的粒径和Zeta电位分别为(118.2±4.6)nm和(31.6±4.9)m V;载药量和包封率分别为(6.5±0.2)%和(96.2±1.8)%;血清中48 h累积泄漏率30%,稳定性良好;YM的细胞摄取量是普通长循环脂质体(CM)的10倍,IC50与CM相比显著降低(P0.05),体内抑瘤率为58.8%,显著高于CM组的42.7%。结论:YM稳定性良好,具有较好的体内外抗肿瘤活性。
[Abstract]:Aim: to prepare mitoxantrone invisibility cationic liposome (YM) and study its preparation properties and anti-tumor effect in vitro and in vivo. Methods: the membrane materials were prepared by ammonium sulfate gradient method using 2-dioleyl hydroxypropyl -3-N (N-N) N-trimethylammonium chloride (DOTAP) and polyethylene glycol 2000- dicarbonyl phosphatidylethanolamine (DSPE-PEG2000) as positive and invisible membranes, respectively. The stability of B16F10 cells was investigated by high intension scanner, and its uptake in B16F10 cells at 2 h was investigated. MTT assay was used to determine the effect of B16F10 on the proliferation of B16F10 cells and the anti-tumor effect of B16F10 subcutaneous transplanted tumor model was studied in vivo. Results the particle size and Zeta potential were (118.2 卤4.6) nm and (31.6 卤4.9) MV, the drug loading and entrapment efficiency were (6.5 卤0.2)% and (96.2 卤1.8), respectively. The tumor inhibition rate in vivo was 58.8%, which was significantly higher than that in CM group (42.7%). Conclusion: ym has good stability and anti-tumor activity in vivo and in vitro.
【作者单位】：四川大学华西药学院;华西医院生物治疗国家重点实验室/生物治疗协同创新中心;
【基金】：第五十四批中国博士后科学基金会资金(编号:2013M542421) 第7批中国博士后科学基金会资金
【分类号】：R944

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