响应面设计优化超临界CO_2法制备盐酸小檗碱脂质体的处方工艺

目的采用中心复合设计实验优化超临界CO2法制备盐酸小檗碱脂质体的处方工艺。方法考察药脂质量比和磷脂质量浓度对盐酸小檗碱脂质体包封率的影响,采用中心复合设计实验对超临界制备盐酸小檗碱处方工艺进行优化,并利用响应曲面法进行优化分析。结果最优的工艺条件为:药脂质量比为13.2∶60,磷脂质量浓度为30 g.L-1,理论包封率为73.30%,载药量为15.98%。在此条件下的实际包封率为(72.15±1.9)%,载药量为15.74%,接近理论预测值。结论作者研究的超临界CO2法制备盐酸小檗碱脂质体,实现了包封率与载药量的最佳组合,且工艺简单,适合工业生产。

Response surface methodology optimization of formulation using supercritical CO2 to prepare berberine liposome

Objective To develop a procedure to prepare and characterize berberine liposome using supercritical CO2.Methods The investigation of drug to phospholipid ratio(m∶ m)and the concentration of soya phosphatidyl choline(SPC)on berberine hydrochloride liposome entrapment efficiency influence were studied to get the range of critical factors and then optimized by central composite design experiment using response surface methodology(RSM)to get the maximum entrapment efficiency and drug loading.Results The optimal formulation was as follow:the ratio of the amount of drug to phospholipid was 13.25∶ 60,and the concentration of soya phosphatidyl choline(SPC)was 30 g · L-1,15.74% berberine was loaded on liposomes and the entrapment efficiency reached 72.15%.Conclusions The preparation of berberine hydrochloride liposome by using supercritical CO2 technology is proved to be the optimal combination both for entrapment efficiency and drug loading.The procedure is simple and suitable for the industrial production.