S/O/W法制备氟尿嘧啶缓释微球及其体外释药行为考察

Preparation and In Vitro Release Behavior of 5-Fluorouracil Loaded Sustained Release Microspheres by S/O/W Method

目的制备包封率较高的氟尿嘧啶聚己内酯微球并研究不同粒径载药微球的性质。方法采用S/O/W乳化溶剂挥发法,考察了微球制备工艺中药物分散方法与油相溶剂的挥发速度对微球包封率的影响。将微球筛分后考察不同粒径微球的载药量及体外释药行为,并用扫描电子显微镜观察释药前后微球的表面形态。结果采用优化工艺条件,制得平均包封率为69.3%的微球;药物缓释达9d以上,释药前后微球表面形态无明显变化。结论S/O/W乳化溶剂挥发法制备得到包封率较高、具有缓释特性的氟尿嘧啶聚己内酯微球。

OBJECTIVE To prepare 5-fluorouracil loaded polycaprolactone （PCL） microspheres and study the characteristics of microspheres within different sizes. METHODS Microspheres were prepared by a S/O/W emulsion/solvent evaporation method. The effects of dispersing methods and the evaporation rate of organic solvent on entrapment efficiency were investigated. The microspheres with different sizes were characterized by drug loading, surface morphology and in vitro drug release. RESULTS Microspheres with average entrapment efficiency of 69.3% were obtained under optimized condition. It took more than 9 d for the drug to release completely from the microspheres. There was no obvious change in the surface morphology of microspheres after the drug was completely released. CONCLUSION 5-Fluorouracil loaded sustained release polycaprolactone microspheres with high entrapment efficiency were prepared by S/O/W emulsion/solvent evaporation method.