Preparation and in Vitro Release of 5-FU-PLGA Double Emulsion Microsphere

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Abstract

5-FU-PLGA double emulsion microspheres were prepared by double emulsion solvent evaporation method. Single factor design was used to study the influence of the first phase volume ratio (inner water phase and oil phase) and the second phase volume ratio (the first phase and outer water phase) on the double emulsion. Orthogonal design was used to study the influence of stirring temperature, stirring time, the concentration of excipient and the concentration of carrier in oil phase on the prepared microspheres. And the preparation conditions were optimized. The optimal preparation method was as follows: the first phase volume ratio was 1:2, the second phase volume ratio was 1:1, the stirring temperature was 10 ℃, the stirring time was 6 h, the concentration of excipient and the concentration of carrier in oil phase were 0.5% and 15%, respectively. The prepared microspheres showed perfect sphericity and narrow particle size distribution. The average particle size was 5.20 μm. The drug loading was 5.34%. The encapsulation efficiency was 77.22%. The in vitro release study showed that the 5-FU-PLGA microspheres showed obvious sustained-release effect and the release behavior accorded with Higuchi model.

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	Articles by authors
	Huang Huiling
	Li Yi
	Wang Yue
	Wei Zhenping

Keywords： 5-fluorouracil； emulsion solvent evaporation method； double emulsion microsphere

Received 2013-11-04;

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Huang Huiling, Li Yi, Wang Yue, Wei Zhenping.Preparation and in Vitro Release of 5-FU-PLGA Double Emulsion Microsphere[J] Chemcial Industry and Engineering, 2016,V33(1): 76-81

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