响应曲面法优化姜黄素-原花青素复合磷脂脂质体的制备

Response surface methodology to optimize the preparation of urcumin-proanthocyanidin composite phospholipid liposomes

目的筛选具有协同增效的天然抗氧化剂——姜黄素-原花青素,运用响应曲面法优化姜黄素-原花青素复合磷脂脂质体(curcumin-proanthocyanidins composite phospholipid liposome,Cur-PCCPL)的制备工艺。方法考察大豆卵磷脂(soya phosphatidylcholine,SPC)与氢化大豆卵磷脂(hydrogenated soya phosphatidylcholine,HSPC)的质量比、卵磷脂与胆固醇质量比和药脂质量比对CurPC-CPL包封率的影响,采用Box-Behnken设计实验对逆相蒸发法制备复合磷脂脂质体处方工艺进行优化分析,最后对其形态、粒径、稳定性、抗氧化性进行评价。结果最优的工艺条件为∶SPC与HSPC质量比为8. 73∶1. 00、卵磷脂与胆固醇质量比为7. 10∶1. 00、药脂质量比为1. 00∶30. 65、姜黄素与原花青素的质量比为1∶3。理论包封率:姜黄素为82. 68%、原花青素为68. 65%。在此条件下的实际包封率:姜黄素为81. 74%、原花青素为66. 96%,接近理论预测值。结论复合磷脂脂质体对姜黄素和原花青素的包载提高了复合天然抗氧化剂的稳定性,为协同抗氧化在实际中的应用提供理论依据。

Objective To screen the natural antioxidant with synergistic effect and optimize the preparation of curcumin-proanthocyanidins composite phospholipid liposome by response surface methodology. Methods The investigation of hydrogenated soya phosphatidylcholine to soya phosphatidylcholine ratio,phosphatidylcholine to cholesterol ratio and drug to lecithin ratio on curcumin-proanthocyanidin composite phospholipid liposomes（ Cur-PC-CPL） entrapment efficiency influence were studied to get the range of critical factors and then optimized by Box-Behnken design experiment using response surface methodology（ RSM） to get the maximum entrapment efficiency. Finally,the shape,particle size,stability and antioxidant activity of Cur-PC-CPL were evaluated. Results The optimal formulation was as follow： the quality ratio of SPC to HSPC was 8. 73,the quality ratio of phosphatidylcholine to cholesterol was 7. 10,the quality ratio of drug to lecithin was 1∶ 30. 65 and the quality ratio of the amount of curcumin to proanthocyanidin was 1∶ 3,and the entrapment efficiency of curcumin and proanthocyanidins reached 82. 68% and 68. 65%,respectively. Conclusion The encapsulation of curcumin and proanthocyanidins with composite phospholipid liposomes has improved the stability of natural antioxidant and provided theoretical basis for the practical application of synergistic antioxidation.