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To evaluate the effect of targeting to hepatoma treated by magnetic biliary stent combining with magnetic nanoparticle containing 5-fluorouracil (5-FU), thirty-two nude mice modes with transplanted hepatoma were divided equally into four groups randomly. Experimental group received magnetic biliary stent and magnetic nanoparticles containing 5-FU. The tumor volume and pathomorphology of all groups was measured. The tumor control rate of the experimental group provided magnetic biliary stent wires and magnetic nanoparticles containing 5-FU is remarkably higher than three other control groups, showing significant curative effect. More apoptosis of tumor cells could be detected easily in experimental group. There are more apoptotic bodies and phagotrophic magnetic particle in apoptosis cells of experimental group under electron microscope. Magnetic biliary stent combining with magnetic nanoparticle containing 5-FU could inhibit the growth of hepatoma, and its curative effect is more remarkable than the traditional methods based on extal magnetic fields.