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目的为了提高齐墩果酸的生物利用度和靶向性,以卵磷脂和胆固醇为包封材料,研究齐墩果酸脂质体的处方和制备工艺。方法采用薄膜超声分散法制备脂质体,用高效液相法(HPLC)测定齐墩果酸的含量。以包封率为指标,采用星点设计-效应面法优选处方和工艺。结果齐墩果酸脂质体的最佳处方和工艺条件为:卵磷脂与胆固醇的质量比为7;卵磷脂与齐墩果酸的质量比为5.5,超声时间为35 min。制备的脂质体平均粒径为312 nm,平均包封率为90.66%。结论该工艺方法简便、稳定可行,适用于齐墩果酸长循环脂质体的制备。
Objective To improve the bioavailability and targeting of oleanolic acid, lecithin and cholesterol as encapsulating materials were used to study the formulation and preparation of oleanolic liposomes. Methods Liposomes were prepared by ultrasonic dispersion method and the content of oleanolic acid was determined by high performance liquid chromatography (HPLC). The entrapment efficiency as an indicator, the use of star design - response surface method of prescription and process optimization. Results The optimal prescription and technological conditions of oleanolic liposomes were as follows: the mass ratio of lecithin to cholesterol was 7; the mass ratio of lecithin to oleanolic acid was 5.5; the time of ultrasound was 35 min. The prepared liposomes had an average particle size of 312 nm and an average entrapment efficiency of 90.66%. Conclusion The method is simple, stable and feasible, suitable for the preparation of oleanolic acid long circulating liposomes.