阿霉素纳米粒的制备及其载药性能的响应面分析

Preparation of Doxorubicin-loaded nanoparticles and optimization of the loading perform ance with response surface methodology

目的制备阿霉素纳米粒,并对其载药性能进行响应面优化。方法采用溶剂去除法制备阿霉素纳米粒,用HPLC-荧光检测法测定阿霉素含量,表征纳米粒,通过响应面法优化影响阿霉素纳米粒载药性能的不同因素。结果制备的阿霉素纳米粒粒径小,圆整度好,分布较均匀;采用Box-Behnken试验设计法,研究各因素及其交互作用对纳米粒载药性能的影响,利用Design-Expert 8.0软件对实验数据进行回归分析,得到二次数学模型方程,确定最佳条件为乳化剂2.50%、阿霉素6.50 mg、聚乙烯吡咯烷酮10%。结论在最佳条件下,纳米粒的包封率为85.11%±2.17%,载药量为2.89%±0.09%。

OBJECTIVE To prepare Doxorubicin -loaded nanoparticles （DNL） and optimize the loading performance with response surface methodology. METHODS DNL were prepared by solvent removal method. DNL were characterized by HPLC - scanning electron microscopy （SEM） for morphological properties and laser light scattering （LLS） for size and size distribution. And response surface methodology （RSM） was used to optimize the loading performance of DNL. RESULTS Nanoparticles exhibited a spherical shape and a narrow distribution. The Box - Behnken design was applied and the interactions of each factor on loading performance were also investigated by Design - Expert 8.0. The optimum conditions were emulsifier concentration of 2.50% , Doxorubicin inputs of 6.5 mg and polyvinylpyrrolidone concentration of 10%. CONCLUSION The encapsulation efficiency of DNL was 85. 11%±2. 17% and drug loading was 2. 89%±0.09% under the optimum conditions.