葛根素PEG-PE纳米胶束的制备及降低红细胞溶血的初步研究  

Preparation of Puerarin-loaded PEG-PE Nano-micelle and Its Reducing Hemolysis Effect

作　　者：方瑞华[1] 梁卫青[1] 张佳军[1] 

机构地区：[1]浙江中医药大学附属嘉兴中医院,浙江嘉兴314001

出　　处：《中国现代应用药学》2016年第9期1147-1152,共6页Chinese Journal of Modern Applied Pharmacy

摘　　要：目的采集葡萄糖-6-磷酸脱氢酶(glucose-6-phosphate ehydrogenase deficiency,G6PD)缺陷的动物模型血液,评价葛根素PEG-PE纳米胶束降低红细胞溶血的作用。方法 1%乙酰苯肼皮下注射大鼠制备G6PD缺陷的动物模型,取其红细胞制成混悬液,比较评价葛根素和葛根素PEG-PE纳米胶束的溶血作用、红细胞脆性及红细胞膜流动性。结果葛根素出现了明显的红细胞溶血,且随着浓度变化和孵育时间延长具有增加的趋势,溶血率高达38%,而葛根素PEG-PE纳米胶束未见明显溶血;另外,红细胞脆性实验结果表明,葛根素PEG-PE纳米胶束对红细胞膜的作用非常轻微,H50%为(42.1±1.1)%,显著小于葛根素的该数值(53.1±1.2)%,红细胞膜流动性结果表明,葛根素PEG-PE纳米胶束对红细胞膜的流动性影响非常轻微。结论葛根素PEG-PE纳米胶束良好的血液相容性,为该药物的体内研究和进一步新型药物制剂开发奠定基础。OBJECTIVE To explore and analyze the reducing hemolytic effects of puerarin-loaded PEG-PE nano-micelle via the glucose-6-phosphate dehydrogenase（G6PD）-deficient rats blood. METHODS The rat model with G6PD-deficiency was established via injecting 1% acetylphenyl-hydrazine. Then the G6PD-deficient erythrocyte suspension obtained from this rat model was used to evaluate the hemolytic effects of PUE and puerarin-loaded PEG-PE nano-micelle via hemolytic activity, erythrocyte osmotic fragility assay and membrane fluidity of erythrocytes. RESULTS PUE could cause a serious hemolysis to the erythrocyte suspension with the increase of drug concentration and the prolongation of drug incubation time, the hemolytic rate of PUE was up to 38%, while PEG-PEN revealed no significant hemolysis. Additionally, the result of erythrocyte osmotic fragility indicated that puerarin-loaded PEG-PE nano-micelle exerted a slight effect on the erythrocyte membranes, its H50% was（42.1±1.1）%, much less than that（53.1±1.2）% of PUE. Erythrocyte membrane fluidity indicated that the effect of puerarin-loaded PEG-PE nano-micelle on erythrocyte membrane fluidity was very slight. CONCLUSION The good blood compatibility of puerarin-loaded PEG-PE nano-micelle makes it a favorable candidate for in vivo tests and puerarin-loaded PEG-PE nano-micelle can also provide the useful insight for the further formulation development as an innovative drug.

关 键 词：葛根素PEG-PE纳米胶束 红细胞溶血 红细胞脆性 红细胞膜流动性 

分 类 号：R944.5[医药卫生—药剂学] R965.2[医药卫生—药学]