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采用乙醇注入法制备齐墩果酸冻干脂质体,再用自制的三甲基壳聚糖进行表面修饰。通过比较冻干品外观、冻干前后理化性质变化,筛选最优冻干工艺、冻干保护剂种类与用量。结果表明,以6%海藻糖为冻干保护剂,经-80℃速冻6 h,冷冻干燥30 h,可得到外观良好、易重建的冻干脂质体。冻干前后药物包封率为(96.8±1.7)%和(97.1±0.9)%,平均粒径为(164.0±4.2)和(195.5±5.9)nm,ζ电位为(23.8±0.2)和(20.3±1.1)mV。采用四氯化碳致小鼠急性肝损伤模型考察制品对生化指标的改善作用。与模型组相比,本品可明显降低小鼠血清丙氨酸转氨酶、门冬氨酸转氨酶和肝组织丙二醛水平,对急性肝损伤的保护作用明显。
Oleanolic acid lyophilized liposomes were prepared by ethanol injection and then surface-modified with homemade trimethyl chitosan. By comparing the appearance of freeze-dried products, changes in the physical and chemical properties before and after lyophilization, screening the optimal lyophilization process, lyoprotectant types and dosage. The results showed that freeze-dried liposomes with good appearance and easy reconstitution were obtained by freeze-drying at -80 ℃ for 6 h and freeze-drying for 30 h with 6% trehalose as lyoprotectant. The encapsulation efficiency was (96.8 ± 1.7)% and (97.1 ± 0.9)%, and the mean diameters were (164.0 ± 4.2) and (195.5 ± 5.9) nm and the zeta potential were (23.8 ± 0.2) and ± 1.1) mV. Acute liver injury model induced by carbon tetrachloride was used to investigate the effect of the product on the improvement of biochemical indexes. Compared with the model group, this product can significantly reduce the serum levels of alanine aminotransferase, aspartate aminotransferase and liver MDA levels, and have a significant protective effect on acute liver injury.