丙交酯
共聚物
聚合物
材料科学
乳状液
碳酸三甲烯
溶剂
PLGA公司
粒径
微粒
高分子化学
剂型
毒品携带者
化学工程
核化学
药物输送
化学
色谱法
有机化学
纳米颗粒
纳米技术
复合材料
工程类
作者
K. J. Zhu,J. X. Zhang,C. Wang,Hajime Yasuda,Akiko Ichimaru,Kazumitsu Yamamoto
标识
DOI:10.3109/02652040309178084
摘要
A modified oil-in-oil (o/o) emulsion solvent evaporation technique was adopted to prepare 5-fluorouracil (5-Fu)-loaded poly (L-lactide) (PLLA) or its carbonate copolymer microspheres. The disperse phase was a drug:polymer solution using a solvent mixture of N, N-dimethylformamide (DMF) and acetonitrile and the continuous phase was liquid paraffin containing 1–10% (w/v) Span 80®. The effects of preparative parameters, such as the composition of the inner oil phase, drug:polymer ratio, polymer concentration and agitation rate, on 5-Fu entrapment efficiency and microsphere characteristics were investigated. By introducing 25% (v/v) DMF into the inner oil phase, microspheres with high drug entrapment efficiency and an ameliorated burst effect were achieved. Using this modified method, microspheres with various particle sizes could be produced with a high 5-Fu entrapment efficiency (about 80%). In vitro drug release tests showed a burst release of 5-Fu from PLLA microspheres, followed by a sustained release over 50 days. In the case of poly (L-lactide-co-1,3-trimethylene carbonate) (PLTMC) and poly (L-lactide-co-2,2-dimethyl-1,3-trimethylene carbonate) (PLDTMC), the drug release could be continued for over 60 days.
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