Combined targeted
drug delivery and sustained drug release, through
the application of nanomedicine, show great potential in cancer therapy
and diagnostics. Systems based on folic acid conjugated with graphene
oxide-based magnetic nanoparticles (NPs) show distinct advantages
for such chemotherapeutic applications. Herein, we prepared FA-Fe3O4@nGO-DOX magnetic nanoparticles (MNPs) with a
uniform size distribution based on nanoscale graphene oxide (nGO)
encapsulated Fe3O4, which was conjugated with
folic acid (FA) and loaded with doxorubicin (DOX). The prepared MNPs
were characterized by various biophysical methods and featured a uniform
size distribution. The uniform size of the nGO resulted in a relative
narrow size distribution of the Fe3O4@nGO MNPs,
which contributed to the stability of the nanocarrier system. Cell
viability and in vitro biocompatibility studies of the FA-Fe3O4@nGO-DOX NPs revealed their selective uptake by MGC-803
cells. The relative viability was maintained at ∼90% after
48 h of incubation, and the hemolysis ratio confirmed the low toxicity
of our modified NPs. The pH-controlled drug release and selective
uptake of FA-Fe3O4@nGO NPs by MGC-803 cells
via the FA receptor ensured selective killing of tumor cells. Furthermore,
the nanoparticles for magnetic resonance imaging were analyzed in
vitro and their signal intensity decreased as the NP concentration
was increased. The nanocomposite was highly effective for in vivo
imaging. Additionally, our in vivo antitumor activity and histological
analysis confirmed the selective anticancer activity of the FA-Fe3O4@nGO-DOX NPs. Notably, our NPs were highly active
and mice treated with FA-Fe3O4@nGO-DOX showed
lower weight loss compared with mice treated with Fe3O4@nGO-DOX. More necrotic tissue was observed in the tumors
of the FA-Fe3O4@nGO-DOX group compared with
those observed in the control, Fe3O4@nGO-DOX,
and DOX groups. Thus, FA-Fe3O4@nGO-DOX is an
effective and stable candidate for targeted drug delivery.