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以Pluronic P123为载体材料,采用固体分散-水化法制备包载四乙酰芍药苷(1)的聚合物胶束,以星点设计-效应面法优化处方。优化所得胶束包封率为97.4%、载药量为10.5%、平均粒径为20.5 nm;胶束中1溶解度是原药的585倍。采用线栓法建立大鼠局灶性脑缺血-再灌注(ischemia-reperfusion,I/R)损伤模型。聚合物胶束显著增加了1在I/R损伤大鼠脑内,特别是脑缺血侧的蓄积量,降低了40%的脑部梗死总面积,显著改善了脑损伤神经行为学评分。结果表明1聚合物胶束有效克服了芍药苷的生物药剂学缺陷和1注射液采用增溶剂的刺激性问题,取得预期对脑缺血再灌注损伤的神经保护作用。
Polymeric micelles containing tetraacetylpaeoniflorin (1) were prepared by solid dispersion-hydration method using Pluronic P123 as carrier material, and the prescription was optimized by the method of apical design-response surface method. The optimized micelle size was 97.4%, and the drug loading was 10.5%. The average particle size was 20.5 nm. The solubility of micelles was 585 times higher than that of the original drug. A rat model of focal cerebral ischemia-reperfusion (I / R) injury was established by thread occlusion. Polymeric micelles significantly increased 1 accumulation in the brain, especially in the ischemic area of I / R injured rats, reduced the total area of cerebral infarction by 40%, and significantly improved the neurobehavioral score of brain injury. The results showed that 1 polymer micelles effectively overcome the biopharmaceutical defects of paeoniflorin and irritation of 1 injection with solubilizer, and achieved the neuroprotective effect expected from cerebral ischemia-reperfusion injury.