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

Abstract

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 Fe₃O₄/RGO-PEI as MTX carriers for targeted anticancer therapy. In which, the Fe₃O₄ provided magnetic response properties; RGO acted as a stage for Fe₃O₄ loading and improved the dispersion of Fe₃O₄; polyethylenimine (PEI) was used as a surface modifier and a storehouse for MTX. The prepared Fe₃O₄/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 Fe₃O₄/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 Fe₃O₄/RGO-PEI-MTX exhibited high anticancer activity while low toxicity to normal cells, and also the Fe₃O₄/RGO-PEI composites were practically non-toxic. Thus, our results revealed that Fe₃O₄/RGO-PEI-MTX would be a competitive candidate for targeted delivery and controlled release of MTX.

Keywords:

• Reduced graphene oxide
• Fe₃O₄
• polyethylenimine
• methotrexate
• pH-sensitive
• targeted cancer therapy

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

The authors are grateful for the National Nature Science Foundation of China (No. 51902141, 51872129), the Natural Science Foundation of Jiangsu Province (No. BK20191038), the Applied Fundamental Research Project of Changzhou (No. CJ20210072), the Talent Introduction Project of Jiangsu University of Technology (No. KYY17021).