星点设计-响应面法优化石杉碱甲二元醇质体处方及其理化性质考察

Optimization of the Formulation of Huperzine A Binary Ethosomes by Central Composite Design-response Surface Methodology and Its Physicochemical Properties

关键词:  石杉碱甲  二元醇质体  处方优化  星点设计-响应面法

Key words:  huperzine A  binary ehosomes  prescription optimization  central composite design-response surface method

摘要:

目的 优化石杉碱甲二元醇质体的处方，并对其理化性质进行考察。方法 采用注入法制备石杉碱甲二元醇质体。以卵磷脂含量(X₁)、无水乙醇含量(X₂)、混合醇含量(X₃)为考察因素，以包封率(Y₁)与平均粒径(Y₂)为评价指标，通过星点设计-响应面法优化醇质体处方。并考察醇质体的粒径、电位等理化性质。结果 优选的处方为卵磷脂含量3.60%，无水乙醇含量22.50%，混合醇含量45.00%，在此条件下，石杉碱甲二元醇质体的平均包封率为(94.05±0.22)%，平均粒径为(260.1±5.7)nm，Zeta电位为(-20.9±0.3)mV，PDI值为0.188±0.056。结论 星点设计-响应面法建立的响应方程具有较好的预测性，可用于石杉碱二元醇质体处方的优化，所得二元醇质体性质稳定。

Abstract:

OBJECTIVE To optimize the formulation of huperzine A binary ethosomes and investigate its physicochemical properties. METHODS The injection method was used to prepare huperzine A binary ethosomes. Taking lecithin content(X₁), absolute ethanol content(X₂) and mixed alcohol content(X₃) as the inspection factors, central composite design-response surface method and overall desirability were used to optimize the formulation with the encapsulation efficiency(Y₁) and average particle size(Y₂) as evaluation indicators. The physicochemical properties of ethosomes such as particle size and potential were investigated. RESULTS The optimum preparation of formulation were the lecithin content of 3.60%, the absolute ethanol content of 22.50% and the mixed alcohol content of 45.00%. Under these conditions, the average encapsulation efficiency was (94.05±0.22)%, the average particle size was (260.1±5.7)nm, the Zeta potential was (-20.9±0.3)mV and the PDI was 0.188±0.056. CONCLUSION The response equation established by central composite design-response surface method has good predictability, and can be used to optimize the formulation of huperzine A binary ethosomes. The obtained ethosomes have stable properties.