鬼臼毒素-固体脂质纳米粒的制备及质量考察

Preparation and quality evaluation of solid lipid nanoparticles containing podophyllotoxin

目的:探讨鬼臼毒素-固体脂质纳米粒的制备方法及其质量。方法:实验于2005-12/2006-08在南方医科大学药学部实验室完成。在制备工艺研究上进行单因素考察和正交实验设计优化处方,以鬼臼毒素-固体脂质纳米粒粒径大小和Zeta电位、形态学、包封率、pH值作为样本质量考察指标,最终确定以改良的乳化蒸发-低温固化法制备鬼臼毒素-固体脂质纳米粒。实验评估:①用透射电镜考察纳米粒的形态。②用粒径分析仪检测纳米粒粒径大小和Zeta电位。③用高效液相色谱法测定纳米粒中鬼臼毒素的包封率。④用pH计测定鬼臼毒素-固体脂质纳米粒混悬液的pH值。结果:①鬼臼毒素-固体脂质纳米粒形态:基本呈圆形或椭圆形。②粒径大小和Zeta电位:分别为(75.3±26.2)nm,(23.2±3.1)mV。③包封率:86.4%。④pH值:4.66±0.18。结论:鬼臼毒素-固体脂质纳米粒制备工艺简单,考察制剂质量较理想。

AIM： To investigate the technological process of preparation and quality of the solid lipid nanoparticles （SLN） containing podophyllotoxin （PPT）. METHODS： The experiment was performed in the Laboratory of Pharmacy Department at Southem Medical University from December 2005 to August 2006. SLN containing PPT was prepared using the method of modified emulsion evaporation at a high temperature and solidification at a low temperature, the morphology of particles was examined by transmission electron microscope. The particle size, zeta potential, morphology, trapment efficiency and pH value of PPT in the nanoparticles were determined by particle size analyzer and high performance liquid chromatography, respectively. RESULTS： （1）PPT-SLN appeared as round or ellipse shape.（2）The mean diameter of particles and Zeta potential of PPT in the nanoparticles were （75.3＋26.2） nm and （23.2＋3.1） mV.（3）The entrapment efficiency was 86.4%.（4）pH value： 4.66＋0.18. CONCLUSION： SLN-PPT can be prepared in simple way, and the resulting medicated nanoparticles have a good quality.