Box-Behnken Design-响应面优化法优化芍药总苷脂质体的制备工艺及体外释放研究

Optimization of preparation technology for total glucosides from Paeonia lactiflora liposome by BBD-RSM and its in vitro release

目的研究芍药总苷(TGP)脂质体的最佳制备工艺及其体外释放情况。方法采用逆向蒸发法制备TGP脂质体,以包封率为评价指标,采用Box-Behnken Design-响应面优化法(BBD-RSM)优化最佳制备工艺参数,并对其体外释放情况进行考察。结果最佳处方为胆固醇与磷脂质量比为1∶2.7,TGP与脂类质量比为1∶29,水化介质用量5.1 m L,药物的平均包封率为73.0%,体外12 h累积释放率为42.18%。结论 TGP脂质体制备工艺合理可行,包封率高,稳定性好,有良好的缓释作用。

Objective To optimize the preparation technology for total glucosides from Paeonia lactiJlora （TGP） liposome and study on its in vitro release. Methods Liposomes were prepared by reverse-phase evaporation technique. Taking the entrapment efficiency （EE） as indexes, the preparation of liposome was optimized using Box-Behnken design-response surface method （BBD-RSM）, and the in vitro release was studied. Results The optimal formulation was cholesterol-lecithin （1 ：2.7）, TGP-lipid （1 ： 29）, and hydrated medium of 5.1 mL. The average EE were 73.0% and the 12 h in vitro accumulative release rate was 42.18%. Conclusion The optimized process is rational and feasible, and the TGP liposome has the higher EE and good stability with better sustained release in vitro.