去甲斑蝥素白蛋白纳米粒的制备及质量评价  

Preparation and Quality Evaluation of Norcantharidin Albumin Nanoparticles

作　　者：朱钰叶[1] 张玲 

机构地区：[1]咸阳职业技术学院医学院,陕西咸阳712000 [2]咸阳市中心医院

出　　处：《中国药师》2018年第3期420-425,共6页China Pharmacist

摘　　要：目的:制备去甲斑蝥素白蛋白纳米粒,并考察其理化性质。方法:采用超高压微射流技术制备去甲斑蝥素白蛋白纳米粒,以白蛋白纳米粒的平均粒径和药物包封率作为评价指标,首先应用Plackett-Burman试验设计法筛选出对白蛋白纳米粒性质影响显著的处方和工艺变量,再通过Box-Behnken试验设计法对筛选的变量进一步优化。考察了去甲斑蝥素白蛋白纳米粒的外观形态、粒径分布和Zeta电位及体外释药行为。结果:通过优化制备的去甲斑蝥素白蛋白纳米粒呈类球形分布,平均粒径为(105.2±30.1)nm,PdI为0.127,Zeta电位为(-24.7±1.9)mV,在0.5%吐温80磷酸盐缓冲液(pH 7.4)中24 h的累积释放度为81.4%。结论:采用超高压微射流技术制备去甲斑蝥素白蛋白纳米粒,工艺简便可行,重复性好,有望工业化生产。Objective： To prepare norcantharidin albumin nanoparticles and evaluate the physical characteristics of the albumin nanoparticles. Methods： Norcantharidin albumin nanoparticles were prepared by ultra-high pressure microfluidization technology. The average particle size and the drug entrapment efficiency of albumin nanoparticles were used as the evaluation indices. Firstly,PlackettBurman experimental design was used to screen the formula and process variables which had significant effects on the properties of albumin nanoparticles,and then Box-Behnken experimental design was used to optimize the variables range. The morphology,particle size distribution,zeta potential and in vitro drug release behavior were investigated. Results： The average particle size of norcantharidin albumin nanoparticles was（ 105. 2 ± 30. 1） nm,the PdI was 0. 127,and the zeta potential was（-24. 7 ± 1. 9） mV. In 0. 5% Tween-80 phosphate buffered saline（ pH 7. 4）,the in vitro cumulative release of norcantharidin albumin nanoparticle suspension reached up to 81. 4% in 24 h. Conclusion： The preparation technology of norcantharidin albumin nanoparticles by ultra-high pressure microfluidization technology is simple and feasible. The preparation technology can be used in industrial production.

关 键 词：去甲斑蝥素 白蛋白纳米粒 超高压微射流技术 Plackett-Burman试验设计 BOX-BEHNKEN试验设计 

分 类 号：R944.9[医药卫生—药剂学]