Mangiferin is a promising effective chemopreventiveagent against various tumors. However, itsclinical use is limited by poor water solubility and lowbioavailability. In this article, mangiferin loaded magneticPCEC microspheres (MG-MS) were designed, characterizedand the antitumor activity of MG-MS was evaluatedin vitro. The magnetic nanoparticles (MNP) were synthesizedvia the high-temperature reaction of ironacetylacetonate in phenyl ether in the presence of oleic acidand oleylamine. Poly (ε-caprolactone)-poly (ethyleneglycol)-poly (ε-caprolactone) (PCL-PEG-PCL, PCEC)copolymers were formed by ring-opening copolymerizationof ε-CL initiated by PEG-diol using Sn(Oct)2 as acatalyst and MG-MS were prepared by solvent diffusionmethod. MNP, PCEC copolymer, and MG-MS werecharacterized by GPC, TEM, XRD, FT-IR, 1H-NMP andMalvern Laser Particle Sizer. Meanwhile, the antiproliferativeactivity in vitro and in vitro release behavior of thismicrospheres were studied in detail. The results indicatethat the obtained magnetic microspheres might have greatpotential as an effective carrier for mangiferin used incancer chemotherapy.