Experimental study of 5-fluorouracil loaded polylactic acid nanoparticles control-releasing preparation on tumor

AIM: To investigate the preparation techniques and anti-tumor effects both in vitro and in vivo of a novel nanoparticles control-releasing preparation of 5-fluorouracil (5-FU) by intravenous injection.METHODS: With polylactic acid (PLA) as marix materials,we adopted ultrasound emulsification method to prepare PLA enveloped 5-FU nanoparticles (5-FU-NPs).Scanning electricity microscopy was used to observe the morphology of 5-FU-NPs and laser optical scattering experiment was conducted to determine its diameter distribution.The drug-carrying capacity (ratio) of the nanoparticles was determined by means of high-power liquid chromatography(HPLC) and MTT test was used to observe cytotoxicity in vitro.The anti-tumor effects were determined at different dosages,frequencies of taking drugs in vivo.RESULTS: Scanning electron microscopy showed that the 5-FU-NPs were globular particles with smooth surface in an average particle diameter of 191.9 nm with a normal distribution,and the drug-carrying capacity of 5-FU-NPs was 15.2%.5-FU-NPs had the same anti-cancer effect as unenveloped drug in vitro and showed typical dose-effect relationship.Compared to naked 5-FU,5-FU-NPs presented significant difference (P<0.05) in anti-cancer effect.CONCLUSION: Nanoparticles may serve as effective carrier for controlled release of 5-FU,which lead to reasonable administration of 5-FU with less toxicity.