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溶剂扩散法制备聚乙二醇修饰积雪草酸(asiatic acid,AA)纳米结构脂质载体(pegylated asiatic acid loaded nanostructured lipid carriers,p-AA-NLC),并结合星点设计-效应面法得到p-AA-NLC的最优处方工艺,其中PEG/脂质为8.0%,AA/脂质为22.0%,该条件下的纳米体系荷负电荷(-37.1±0.9)m V,粒径(111.2±2.9)nm,包封率大于90%,载药量适中(15.4±0.2)%。4个指标实验值与模型预测值相比偏差均小于5%,表明实验中建立的模型预测性良好。同时采用大鼠在体肠灌流模型对优化后的p-AA-NLC进行肠吸收考察,药物有效吸收系数(Peff)、吸收速率常数(Ka)等参数评价该亲水性修饰纳米粒的肠吸收情况,结果显示p-AA-NLC组的Peff,Ka较未修饰组有显著提高(P<0.05),提示积雪草酸纳米结构脂质载体(asiatic acid loaded nanostructured lipid carriers,AA-NLC)经亲水性PEG修饰后其小肠吸收有明显的促进作用。
The PEG-modified asiatic acid (AA) nanostructured lipid carriers (p-AA-NLC) were prepared by solvent diffusion method, and p -AA-NLC. The PEG / lipid was 8.0% and AA / lipid was 22.0%. The nanostructures under this condition had a negative charge (-37.1 ± 0.9) m V, a particle size of (111.2 ± 2.9) nm. The entrapment efficiency was more than 90% and the drug loading was moderate (15.4 ± 0.2)%. The deviation of the experimental values of the four indexes from the model predictive value is less than 5%, indicating that the model established in the experiment is of good predictability. At the same time, intestinal absorption of optimized p-AA-NLC was investigated in rat intestinal peritoneal perfusion model, and the parameters of Peff and Ka were evaluated in intestinal absorption of the hydrophilic modified nanoparticles (P <0.05), suggesting that asiatic acid loaded nanostructured lipid carriers (AA-NLC) After water-based PEG modified intestinal absorption was significantly promoted.