聚乙二醇包裹表阿霉素脂质体的制备及评价
发布时间:2018-06-13 16:40
本文选题:聚乙二醇 + 左旋聚乳酸 ; 参考:《首都医科大学学报》2015年02期
【摘要】:目的制备聚乙二醇(polyethylene glycol,PEG)包裹表阿霉素脂质体,对其药剂学性质和活性进行评价。方法采用乳化溶剂挥发法制备聚乙二醇包裹表阿霉素的脂质体,用扫描电镜和透射电镜观察其形态,用激光纳米粒度仪测定粒径分布及Zeta电位、并对包封率、稳定性及体外释药特性进行研究,采用MMT法和S180小鼠模型评价体内外抗肿瘤活性。结果聚乙二醇包裹表阿霉素的脂质体的粒径为(231.4±2.0)nm,动电位为(-25.62±0.68)m V,包封率为(53.14±4.85)%,各项稳定性均有明显提高,体外释放缓慢,小鼠剂量可增加到6μmol/kg,给药间隔可延长至72 h,并显示比表阿霉素好的抗肿瘤活性。结论本实验获得了较理想的聚乙二醇包裹表阿霉素脂质体,体外释药符合长效制剂特征,血浆中稳定,具有p H敏感性,可改善表阿霉素用药安全性,延长药物作用时间。
[Abstract]:Aim to prepare PEG coated epirubicin liposome and evaluate its pharmacological properties and activity. Methods the polyethylene glycol encapsulated adriamycin liposomes were prepared by emulsifying solvent volatilization method. The morphology of the liposomes was observed by scanning electron microscope and transmission electron microscope. The particle size distribution and Zeta potential were measured by laser nano-particle size analyzer, and the encapsulation efficiency was evaluated. The stability and drug release characteristics in vitro were studied. The anti-tumor activity in vivo and in vitro was evaluated by MMT method and S180 mouse model. Results the particle size, dynamic potential and entrapment efficiency of PEG-encapsulated epirubicin liposome were 231.4 卤2.0 nm, 25.62 卤0.68 mg / v and 53.14 卤4.85 mg 路L ~ (-1), respectively. The stability of the liposomes was significantly improved and the release in vitro was slow. The dose of mice was increased to 6 渭 mol / kg, the interval of administration was prolonged to 72 hours, and the antitumor activity was better than that of epirubicin. Conclusion in this experiment, a more ideal PEG-encapsulated epirubicin liposome was obtained. The drug release in vitro was consistent with the characteristics of long-acting preparation, stable in plasma and sensitive to pH, which could improve the safety of epirubicin and prolong the time of drug action.
【作者单位】: 首都医科大学化学生物学与药学院药剂学系;首都医科大学化学生物学与药学院药物化学系;
【基金】:“十二五”重大新药创制科技重大专项(2011ZX09302-007-01)~~
【分类号】:R943
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