维生素A棕榈酸酯冻干脂质体的制备及稳定性

Preparation of vitamin A palmitate(VAP) freeze-dried liposomes and study of its stability

目的制备维生素A棕榈酸酯(VAP)冻干脂质体,并对其稳定性进行研究。方法用薄膜分散法制备维生素A棕榈酸酯脂质体,用正交设计法优化处方和制备工艺。以50 g·L-1海藻糖-50 g·L-1蔗糖(质量比1∶1)为冻干保护剂进行冻干。采用HPLC法测定VAP脂质体中维生素A棕榈酸酯的含量及包封率。结果 VAP脂质体冻干前平均粒径为(90.06±2.88)nm,zeta电位为-(5.08±0.18)m V,平均包封率为(90.06±1.73)%,冻干后复溶平均粒径为(83.40±0.78)nm,zeta电位为-(3.65±0.86)m V,平均包封率为(90.84±0.80)%。VAP冻干脂质体在4℃保存3个月稳定。结论以最佳处方和工艺制备的VAP脂质体包封率高、重现性好。VAP冻干脂质体对光照和高温不稳定,应避光储存在4℃冰箱中。

Objective To prepare vitamin A palmitate(VAP) freeze-dried liposomes and study its stability. Methods The thin film dispersion method was used to prepare VAP liposomes and the orthogonal design method was employed to optimize the prescription and preparation technology. 50 g·L-1 trehalose and 50 g·L-1sucrose(1∶1) was used as protective agent of freeze-drying. High performance liquid chromatography(HPLC) method was employed to evaluate the content and coating rate of vitamin A palmitate in VAP liposomes. Results Prior to lyophilization, average particle size was(90.06±2.88) nm, zeta potential was –(5.08±0.18) m V, average coating rate at(90.06±1.73)%, after lyophilization, the average particle size was(83.40±0.78) nm, zeta potential was –(3.65±0.86) m V, average coating rate was(90.84±0.80)% of the dissolving liposomes. VAP freeze-dried liposomes was stable at 4 ℃ for 3 months. Conclusion The results showed that encapsulation efficiency of VAP liposomes is high and has a good reproducibility, which was prepared by the optimized formulation and technology. VAP freeze-dried liposome is not stable when exposure to light or at high temperature. It stores at 4 oC in the fridge.