目的:制备呋喃二烯长循环脂质体并进行表征。方法:采用薄膜超声分散法制备呋喃二烯长循环脂质体,以包封率和粒径为评价指标,通过单因素-正交设计优化脂质体处方及工艺。结果:优化后的处方和制备工艺为:水化温度为55℃,磷脂浓度为3.5%,...目的:制备呋喃二烯长循环脂质体并进行表征。方法:采用薄膜超声分散法制备呋喃二烯长循环脂质体,以包封率和粒径为评价指标,通过单因素-正交设计优化脂质体处方及工艺。结果:优化后的处方和制备工艺为:水化温度为55℃,磷脂浓度为3.5%,磷脂与胆固醇比例为12∶1,脂药比为15∶1,DSPEMPEG2000摩尔百分比为5%。此条件下制备的脂质体包封率为90.6%,平均粒径为113.4 nm,Zeta电位为-45.9 m V。结论:本实验所制备的呋喃二烯长循环脂质体包封率较高,粒度分布范围较窄,平均粒径较小,具有很好的应用前景。展开更多
Aim To prepare 8-chloro-adenosine (8-Cl-A)long circulation liposomes with high entrapped efficiency and prolonged action-time of 8-Cl-A in vivo. Methods To prepare 8-Cl-A long circulation liposomes of nanometer size b...Aim To prepare 8-chloro-adenosine (8-Cl-A)long circulation liposomes with high entrapped efficiency and prolonged action-time of 8-Cl-A in vivo. Methods To prepare 8-Cl-A long circulation liposomes of nanometer size by improved multiple emulsion. The entrapped efficiency, size and size distribution of 8-Cl-A long circulation liposomes were determined, and its pharmacokinetics in rats was evaluated. Results The entrapped efficiency of 8-Cl-A long circulation liposomes was 62.70% and mean diameter of the liposomes was 79.9 nm. The pharmacokinetics studies indicated that 8-Cl-A long circulation liposomes showed higher drug concentration and larger AUC values than that of 8-Cl-A after iv to rats. Conclusion 8-Cl-A long circulation liposomes could prolong the action-time of 8-Cl-A in vivo.展开更多
文摘目的:制备呋喃二烯长循环脂质体并进行表征。方法:采用薄膜超声分散法制备呋喃二烯长循环脂质体,以包封率和粒径为评价指标,通过单因素-正交设计优化脂质体处方及工艺。结果:优化后的处方和制备工艺为:水化温度为55℃,磷脂浓度为3.5%,磷脂与胆固醇比例为12∶1,脂药比为15∶1,DSPEMPEG2000摩尔百分比为5%。此条件下制备的脂质体包封率为90.6%,平均粒径为113.4 nm,Zeta电位为-45.9 m V。结论:本实验所制备的呋喃二烯长循环脂质体包封率较高,粒度分布范围较窄,平均粒径较小,具有很好的应用前景。
文摘Aim To prepare 8-chloro-adenosine (8-Cl-A)long circulation liposomes with high entrapped efficiency and prolonged action-time of 8-Cl-A in vivo. Methods To prepare 8-Cl-A long circulation liposomes of nanometer size by improved multiple emulsion. The entrapped efficiency, size and size distribution of 8-Cl-A long circulation liposomes were determined, and its pharmacokinetics in rats was evaluated. Results The entrapped efficiency of 8-Cl-A long circulation liposomes was 62.70% and mean diameter of the liposomes was 79.9 nm. The pharmacokinetics studies indicated that 8-Cl-A long circulation liposomes showed higher drug concentration and larger AUC values than that of 8-Cl-A after iv to rats. Conclusion 8-Cl-A long circulation liposomes could prolong the action-time of 8-Cl-A in vivo.
