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As one of the well-known anticancer drugs, methotrexate (MTX) has been limited in clinical application due to its side effects on normal tissues. This study focused on the one-step hydrothermal synthesis and  in vitro  evaluation of Fe 3 O 4 /RGO-PEI as MTX carriers for targeted anticancer therapy. In which, the Fe 3 O 4  provided magnetic response properties; RGO acted as a stage for Fe 3 O 4  loading and improved the dispersion of Fe 3 O 4 ; polyethylenimine (PEI) was used as a surface modifier and a storehouse for MTX. The prepared Fe 3 O 4 /RGO-PEI nanocomposites exhibited a suitable size, good stability and magnetic responsibility. And the MTX loading content and loading efficiency were calculated to be 26.6% and 90.5%, respectively. What’s more, due to the diffusion and dissolution of PEI, the Fe 3 O 4 /RGO-PEI-MTX exhibited excellent pH-sensitivity, the values of MTX release rate (%) within 48 h at pH 5.8 and 4.0 were 64.3% and 87.4%, respectively. Furthermore, MTT assays in cancer cells (HepG2) and normal cells (HUVEC) demonstrated that Fe 3 O 4 /RGO-PEI-MTX exhibited high anticancer activity while low toxicity to normal cells, and also the Fe 3 O 4 /RGO-PEI composites were practically non-toxic. Thus, our results revealed that Fe 3 O 4 /RGO-PEI-MTX would be a competitive candidate for targeted delivery and controlled release of MTX.

Synthesis and characterization of magnetic polymeric nanocomposites for pH-sensitive controlled release of methotrexate