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目的制备硬脂醇半乳糖苷修饰的盐酸吉西他滨纳米脂质体(18-GGNL),并采用响应面法优化其处方工艺。方法用硫酸铵梯度法制备18-GGNL,以包封率为评价指标,运用Box-Behnken响应面设计法对处方进行优化,并对其包封率、形态、粒径、稳定性和体外释放度进行综合评价。结果得到最优处方为磷脂与胆固醇的质量比为3.10︰1,硫酸铵浓度0.19 mol·L?1,脂物比为20.99︰1,所得的优化脂质体平均包封率为(70.8±0.95)%,平均粒径为(89.5±5.3)nm,粒径分布较窄,稳定性好且具有缓释特性。结论以硫酸铵梯度法制备的18-GGNL理化性质良好。
Objective To prepare stearyl alcohol galactoside modified gemcitabine nano-liposomes (18-GGNL), and optimize the formulation process by response surface methodology. Methods 18-GGNL was prepared by ammonium sulfate gradient method. The encapsulation efficiency was used as evaluation index, and the prescription was optimized by Box-Behnken response surface design. The encapsulation efficiency, morphology, particle size, stability and in vitro release Conduct a comprehensive evaluation. Results The optimal formulation was obtained as follows: the mass ratio of phospholipid to cholesterol was 3.10︰1, the concentration of ammonium sulfate was 0.19 mol·L -1, the lipid ratio was 20.99︰1, the average entrapment efficiency of the optimized liposomes was (70.8 ± 0.95 )%, The average particle size is (89.5 ± 5.3) nm, the particle size distribution is narrower, the stability is good and the sustained release property is obtained. Conclusion The ammonium sulfate gradient method 18-GGNL good physical and chemical properties.