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

LIU Li-bo,ZHANG Ya-qiong,GUO Sheng-rong* (School of Pharmacy,Shanghai Jiaotong University,Shanghai 200240,China)  
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.
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