载硫酸庆大霉素聚乳酸纳米粒制备的正交设计及体外释药行为研究

Optimization of Preparation Parameters for Gentamicin-loaded PLLA Nanoparticles and the Drug Release Behavior In Vitro

载药纳米粒的制备与应用是纳米生物医学研究中的重要方向之一,要获得释药性能稳定的载药纳米粒,需要解决的一个关键问题是确定重要工艺参数和进行制备工艺的优化。我们运用SPSS软件对复乳法制备载硫酸庆大霉素聚乳酸纳米粒(GS-PLLA-NPs)的工艺条件进行了正交设计优化,通过紫外-可见分光光谱对其体外释放行为进行了测定和分析。实验结果表明,PLLA的浓度与PLLA的分子量是影响GS-PLLA-NPs粒径分布均一性的关键因素,油水相之比对药物的释放行为有显著影响。在优化条件下制备的GS-PLLA-NPs粒径均匀,有较为理想的药物缓释效果,在抗骨术后感染、骨缺损修复等方面具有重要的应用价值。

It has been one of important issues in nanomedicine research field to prepare drug-loaded nanoparticles. Optimization of the preparation parameters plays a key role in obtaining drug-loaded nanoparticles with homogeneous particle size and controlled drug release property. In this paper, gentamicin-loaded PLLA nanoparticles was prepared by means of double emulsion and solvent evaporation technique. Statistical software SPSS was employed to deal with the orthogonal design for optimizing the parameters of the formulation. The in vitro release of gentamicin from nanoparticles was determined by ultra-violet spectroscopy. Analysis of the experimental data based on orthogo- nal design demonstrated that the concentration of PLLA solution and the molecular weight of PLLA had significant influence on the size of nanoparticles, and the ratio of oil phase to water phase exhibited determined role in the gentamicin release property. Gentamicin-loaded PLLA nanoparticles prepared with the optimized parameters showed homogeneous particle size of 277 nm and sustained release property, which displayed a promising potential of clinical applications.