Abstract
Biodegradable poly(lactic-acid) (PLA ) microspheres containing 5-fluorouracil were prepared by a solid in oil in water emulsion solvent evaporation method. The influences of various preparation parameters, such as polymer concentration, polymer molecular weight, oil-phase volume and PVA concentration in the external water phase on the characteristics of the microspheres and drug release profiles, the in vitro cell inhibition were investigated. It was found that the particle size was 100.25 plusmn 2.50 mum and the drug loading was 8.25%(w/w). The in vitro release profiles of 5-fluorouracil loaded microspheres showed an initial burst release and thereafter the release was relatively slow. The in vitro cell inhibition indicate that the activity of 5-Fu is not weakened during the microspheres fabrication process and the solvent evaporation method is a mild fabrication technique for keeping drug stability.
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