Although chemotherapy is regarded as an essential option
in cancer
treatment, it is still far from being perfect. Inadequate tumor drug
concentration and systemic toxicity along with broad biodistribution
have diminished the utility of chemotherapy. Tumor-targeting peptide-conjugated
multifunctional nanoplatforms have emerged as an effective strategy
for site-directed tumor tissues in cancer treatment and imaging. Herein,
Pep42-targeted iron oxide magnetic nanoparticles (IONPs) functionalized
with β-cyclodextrin (ßCD) containing doxorubicin (DOX)
(Fe3O4-ßCD-Pep42-DOX) were successfully
developed. The physical effects of the prepared NPs were characterized
by employing various techniques. Transmission electron microscopy
(TEM) images disclosed that the developed Fe3O4-ßCD-Pep42-DOX nanoplatforms had a spherical morphology and
a core–shell structure with a size of nearly 17 nm. Fourier
transform infrared (FT-IR) spectroscopy showed that β-cyclodextrin,
DOX, and Pep42 molecules were successfully loaded on the IONPs. In vitro cytotoxicity analysis revealed that the fabricated
multifunctional Fe3O4-ßCD-Pep42 nanoplatforms
possessed excellent biosafety toward BT-474, MDA-MB468 (cancerous
cells), and MCF10A normal cells, while Fe3O4-ßCD-Pep42-DOX exhibited great cancer cell killing ability.
The high cellular uptake along with intracellular trafficking of Fe3O4-ßCD-Pep42-DOX highlights the usefulness
of the Pep42-targeting peptide. In vivo results strongly
supported the in vitro results, i.e., significant
tumor size reduction was observed by single-dose injection of Fe3O4-ßCD-Pep42-DOX into tumor-bearing mice.
Interestingly, in vivo MR imaging (MRI) of Fe3O4-ßCD-Pep42-DOX revealed T
2 contrast improvement in the tumor cells and therapeutic
ability in cancer theranostics. Taken together, these findings provided
strong evidence for the potential capability of Fe3O4-ßCD-Pep42-DOX as a multifunctional nanoplatform in cancer
therapy and imaging and opens up a new avenue of research in this
area.