齐墩果酸新型前体脂质体的制备和性质研究

Study on Preparation of a New Oleanolic Acid Proliposomes and Its Properties

目的为了研究齐墩果酸新剂型,制备齐墩果酸新型前体脂质体,并对其体外性质进行考察。方法采用一种新型前体脂质体制备方法将齐墩果酸制成前体脂质体,考察了前体脂质体水合后形成脂质体的形态、粒径、包封率、体外吸收等各项指标,验证了这种新型前体脂质体制备方法制备齐墩果酸脂质体的可行性。结果所形成的齐墩果酸脂质体粒径小、粒度分布均匀,包封率为(85.65±7.96)%。且包封率的大小与脂质体溶液pH、药脂比有关。pH升高,包封率增大,药脂比由5∶1增加到10∶1时,包封率增大。离体小肠吸收实验证明,齐墩果酸脂质体与对照组相比,可显著促进药物吸收。结论新型前体脂质体制备方法可将齐墩果酸制成齐墩果酸脂质体,且形成的脂质体包封率较高,体外促吸收作用良好,此研究为齐墩果酸脂质体的研制奠定了基础。

OBJECTIVE To prepare a new kind of oleanolie acid proliposomes and develop a new formulation of oleanolie acid, and to investigate its properties. METHODS A new kind of proliposome preparation method was used to prepare the oleanolic acid proliposomes, and then the properties of the liposomes, including the surface morphology, the size, the entrapment efficiency and the absorption in vitro,were studied after the proliposomes were changed into the liposomes. RESULTS The study proved the oleanolic acid was trapped into the liposomes. The particle size of the liposomes was small and the size distribution was uniformed, the entrapment effi- ciency was（85. 65 ±7. 96） %. Furthermore, the entrapment efficiency was related to the pH of the liposome solution and the proportion of the drug and the phosphatide （that is P/D）. When pH was increased, the entrapment efficiency was improved. When the proportion of the P/D was increased from 5：1 to 10： 1 ,the entrapement efficiency was increased too. The intestinal absorption result proved that the liposomes contributed to the drug absorption,compared with the control group. CONCLUSION The oleanolic acid can be trapped into the liposomes according to this method. And the entrapment efficiency and the absorption of the liposomes are high. The study will be the first step of the preparation of a new oleanolic acid liposomes.