Preparation of astragaloside Ⅳ liposomes and evaluation of the efficacy in treating ischemic stroke
Objective To optimize the formulation and preparation process of astragaloside Ⅳ liposome,conduct the pharmaceutical evaluation of the liposome,and investigate its therapeutic effect on ischemic stroke in rats.Methods Particle size,polydispersity index(PDI),zeta potential,and encapsulation efficiency were used as investigative factors.Based on above,the formulation and process of astragaloside Ⅳ liposome were optimized by single factor analysis.The quality of astraga-loside Ⅳ liposome was evaluated.The middle cerebral artery embolization surgery was performed using the suture method to establish an ischemic stroke rat model.The mice were divided into sham surgery group,model group,astragaloside Ⅳ group,and astragaloside Ⅳ liposome group.The neurobehavioral changes of the rats,and detect indicators such as brain tissue infarc-tion rate and pathological changes were observed.Results The optimal process parameters were as follows:the mass concen-tration of egg yolk lecithin was 8 mg·mL-1,the ratio of membrane to material was 10∶3,the dosage of astragaloside Ⅳ was 1 mg,hydration temperature was 48 ℃,ultrasound power was 300 W,and ultrasound time was 8 min.The average particle size,PDI,zeta potential,encapsulation efficiency of the prepared astragaloside Ⅳ liposome was(185.97±2.55)nm,0.258±0.012,(-19.91±0.52)mV,and 94.58％±0.67％,respectively.The particle size change of astragaloside Ⅳ liposome was less than 5 nm at 4 ℃ within 7 days.Furthermore,the cumulative release of astragaloside Ⅳ in astragaloside Ⅳ liposome was 39％at 4 h,demonstrating the sustained release effect.In pharmacological experiments,astragaloside Ⅳ liposome could significantly reduce the scores of neurobehavioral deficits and the incidence of brain tissue infarction in rats,as well as reduce pathological chan-ges.Conclusion Astragaloside Ⅳ liposome present small particle size,high encapsulation efficiency,good storage stability,sustained-release properties,and excellent therapeutic effects on ischemic stroke.
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