Box-Behnken响应面法优化益母草碱脂质纳米粒处方  

Formulation Optimization of Leonurine Lipid Nanoparticles by Box-Behnken Response Surface Methodology

作　　者：朱波 ZHU Bo(Hwa Mei Hospital,University of Chinese Academy of Sciences,Ningbo 315010,China)

机构地区：[1]中国科学院大学宁波华美医院,浙江宁波315010

出　　处：《中国现代应用药学》2021年第10期1205-1210,共6页Chinese Journal of Modern Applied Pharmacy

摘　　要：目的制备益母草碱脂质纳米粒并优化处方。方法采用pH梯度结合逆向蒸发法制备益母草碱脂质纳米粒,以粒径、包封率和载药量为评价指标,药物和脂质比例、胆固醇和脂质比例、药物终浓度为考察因素,采用Box-Behnken效应面法优化纳米粒处方,并考察纳米粒体外释放情况。结果益母草碱脂质纳米粒最优处方为药物和脂质比例为9.8%,胆固醇和脂质为1.0%,药物终浓度为10mg·mL-1。制得的纳米粒粒径为(83.9±5.6)nm、包封率(73.3±2.2)%、载药量(4.0±0.0)%,实测值与预测值RSD均<5%。体外释放结果显示,与原料相比,益母草碱脂质纳米粒具有一定的缓释作用。结论 Box-Behnken响应面优化法应用简便、预测性好,所得益母草碱脂质纳米粒包封率和载药量高,符合设计要求。OBJECTIVE To optimize the formulation of leonurine lipid nanoparticles. METHODS The leonurine lipid nanoparticles were prepared by pH-gradients method coupled with reverse evaporation method. Final drug concentration, drug-lipid ratio, cholesterol and lipid ratio were selected as influences factors, the formulation was optimized by Box-Behnken response surface method with particle, the particle size, encapsulation efficiency and loading content as the evaluation parameters. The in vitro release was determined. RESULTS The optimal formulation parameters were as follows: the drug-lipid ratio was 9.8%, cholesterol and lipid ratio was 1.0% and the final drug concentration was 10 mg·mL-1. The mean particle size, entrapment efficiency, and the drug loading were(83.9±5.6)nm,(73.3±2.2)% and(4.0±0.0)%, respectively. RSD of measured and predicted values were all less than 5%. In vitro release test results showed that leonurine lipid nanoparticles had a sustained release effect compared with the raw materials. CONCLUSION The Box-Behnken response surface method is simple and predictable, and have high encapsulation efficiency and drug loading of the obtained leonurine lipid nanoparticles, which meets the design requirements.

关 键 词：益母草碱 pH梯度结合逆向蒸发法 BOX-BEHNKEN效应面法 体外释放 

分 类 号：R284.2[医药卫生—中药学]