石杉碱甲脂质体肌肉注射对小鼠脑缺血模型的长效缓释作用

Huperzine A Liposome Intramuscular Injection on Cerebral Ischemia Mouse Model for Long-term Control Release Effect

目的:小鼠脑缺血再灌注制备缺血性痴呆(AD)动物模型,采用肌肉注射石杉碱甲脂质体(HUPAL),考察石杉碱甲脂质体肌肉注射后对小鼠脑缺血模型的长效缓释作用。方法:采用硫酸铵梯度法制备HUPAL,采用小鼠的脑缺血再灌注为痴呆模型(AD),HUPAL给药后考察实验动物行为学变化,并以大脑皮层乙酰胆碱酯酶水平的高低为评价指标,验证HUPAL的长效缓释作用。结果:采用硫酸铵梯度法制备HUPAL,小鼠脑缺血再灌注动物肌肉注射HUPAL,逃逸潜伏期和逃逸实验中犯错的次数明显降低(P≤0.01)。HUPA溶液剂和HUPAL制剂在同样的给药剂量下,脂质体发挥更长的药理效应。结论:通过硫酸铵梯度法制备的石杉碱甲脂质体(HUPAL),肌肉注射小鼠脑缺血实验动物模型,可以显著延长HUPAL药理作用,达到降低给药次数的目的。

Objective:Animal model of ischemic stroke were developed to test Huperzine A Liposomes controlled release and long time effect.Methods:Huperzine A Liposomes were developed by ammonium sulfate[(NH 4)2 SO 4]gradient,a novel mouse model of subcortical infarcts with dementia.Comparing with HUPA solution,Huperzine A Liposomes muscle tremors and time slobber extent was decreased after administration of HUPA liposomes.According to the results of Morris test,The ability of learning and memory in vascular dementia mice were both enhanced in group HUPA liposomes and group HUPA solution.Results:After intramuscular injection of Huperzine A Liposomes,HUAPLgroup inhibition of acetylcholinesterase percentage were statistically significant compared with the control group.HUPAL 1.0 mg·kg^(-1) group,1,3 days remain a significant inhibitory effect.Other treatment group compared with the control group,no difference in inhibition of acetylcholinesterase percentage.Conclusion:Huperzine A liposome formulation has long-term sustained-release effect and reduces the times of drug administration.