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 mL,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 lactiflora (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.

泸州科技局(2012-S-36);泸州医学院大学生科研项目(201387)