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采用溶剂扩散法制备聚乙二醇修饰的积雪草酸(asiatic acid,AA)纳米结构脂质载体(pegylated asiatic acid loaded nanostructured lipid carriers,p-AA-NLC),以结扎肠循环模型考察其在小肠的吸收分布情况,HPLC检测健康SD大鼠灌胃给予p-AA-NLC后的胆汁药物浓度,间接评价PEG化脂质纳米粒的促口服吸收作用。结果显示,经PEG亲水性修饰的NLC在小肠黏膜的穿透能力大大提高,小肠内的转运量显著增加,大鼠体内药物排泄峰值Cmax较普通纳米粒(asiatic acid loaded nanostructured lipid carriers,AA-NLC)提高了76%,达峰时间tmax减慢,消除半衰期t1/2延长1倍,AUC0→t为AA-NLC组的1.5倍,提示AA-NLC经PEG亲水性修饰后,口服生物利用度显著提高。
Polyethylene glycol-modified asiatic acid loaded nanostructured lipid carriers (p-AA-NLC) were prepared by solvent diffusion method. The absorption and distribution of the drug were measured by HPLC. The concentrations of bile drug in the healthy SD rats after oral administration of p-AA-NLC were measured by HPLC, and the oral absorption of PEGylated lipid nanoparticles was evaluated indirectly. The results showed that the hydrophilicity of PEG modified NLC in the intestinal mucosa significantly increased the penetration capacity of small intestine transport increased significantly, the peak in vivo drug excretion Cmax compared with ordinary nanoparticles (asiatic acid loaded nanostructured lipid carriers, AA- NLC) was increased by 76%, the peak time tmax was slowed down, the elimination half-life t1 / 2 was doubled and the AUC0 → t was 1.5 times that of AA-NLC group, suggesting that the bioavailability of AA- Degree significantly increased.