5-氟尿嘧啶磁性固体脂质纳米粒制备工艺优化研究

Study on Optimization of 5-Fluorouracil Magnetic Solid Lipid Nanoparticles

为提高5-氟尿嘧啶(5-FU)制剂的疗效,降低毒副作用,以单硬脂酸甘油酯为载体,氢化大豆卵磷脂、泊洛沙姆为乳化剂,磁性纳米四氧化三铁为磁体,采用复乳-溶剂挥发法制备5-氟尿嘧啶磁性固体脂质纳米粒(5-FU-MSLN).以包封率为考察指标,通过单因素实验和正交设计对制备工艺进行优化,所制备的5-FU-MSLN包封率为58.35%.用透射电镜观察,磁性固体脂质纳米粒外观形态圆整,粒径分布均匀;在倒置的显微镜下观察,磁性固体脂质纳米粒体外磁响应性良好,实验结果表明,5-FU-MSLN是有希望的静脉给药靶向制剂.

To improve the therapeutic efficacy and reduce the toxicity of 5-Fluorouracil（5-FU）,5-Fluorouracil magnetic solid lipid nanoparticles（5-FU-MSLN） were prepared with a W/O/W double emulsion solvent evaporation technique,using monostearin as the carrier,hydrogenated soybean lecithin and poloxamer as emulsifier,magnetic Fe3O4 nanoparticles as magnets.With the index of encapsulation efficiency,the preparation process was optimized by single-factor test and orthogonal test.As a result,the encapsulation efficiency of 5-FU-MSLN was 58.35%.TEM presented 5-FU-MSLN as spherical particles,evenly distributed;5-FU-MSLN were observed under the inverted microscope,of which vitro magnetic responsiveness was good.Such magnetic solid lipid nanoparticles seem appropriate for vascular administration followed by drug targeting.