Multifunctional magnetic nanoparticles for controlled release of anticancer drug, breast cancer cell targeting, MRI/fluorescence imaging, and anticancer drug delivery

Abstract Anti-cancer drug, free base doxorubicin hydrophobic (DOX-HCL) or paclitaxel (PTX), EPPT-FITC and, oleic acid-Fe 3 O 4 nanoparticles (OA-Fe 3 O 4 ) were incorporated into the tree block PLA-PEG-PLA copolymer. Properties of these nanoparticles, such as structural, magnetic, drug-loading efficiency, drug release kinetics and in vitro cytotoxicity were evaluated in vitro for controlled drug release and targeted drug delivery. Transmission electron microscope (TEM) and dynamic light scattering (DLS) results showed that BMNPs/EPPT/drug have spherical morphology with diameters in the range of 179–203 nm. The release rate of drug from multifunctional nanoparticles was significantly increased with decreasing of the pH. Cytotoxicity assays with drug-loaded nanoparticles were performed in vitro using normal and breast tumor cell lines (MCF12-A and MCF-7 cells respectively), and in vivo evaluating antitumor activity in immunocompetent BABL/c mice. Neither in vitro nor in vivo cytotoxicity was observed for blank nanoparticles. In vitro cytotoxicity assay indicated that the IC50 values of BMNPs/EPPT/drug were significantly lower compared to other nanoparticles. Selectivity of interaction between receptors in breast cancer cells and EPPT peptides of multifunctional nanoparticles resulted in a significant decrease in cell viability in BMNPs/EPPT compared with other nanoparticles. Furthermore, drug-loaded BMNPs/EPPT produced significant decrease of tumor volumes compared with other nanoparticles.