Functional Magnetic Core-Shell System-Based Iron Oxide Nanoparticle Coated with Biocompatible Copolymer for Anticancer Drug Delivery

Abstract

Polymer coating has drawn increasing attention as a leading strategy to overcome the drawbacks of superparamagnetic iron oxide nanoparticles (SPIONs) in targeted delivery of anticancer drugs. In this study, SPIONs were modified with heparin-Poloxamer (HP) shell to form a SPION@HP core-shell system for anticancer drug delivery. The obtained formulation was characterized by techniques including transmission electron microscopy (TEM), Fourier transform infrared spectra (FT-IR), vibration sample magnetometer (VSM), proton nuclear magnetic resonance (1H-NMR), and powder X-ray diffraction (XRD). Results showed the successful attachment of HP shell on the surface of SPION core and the inability to cause considerable effects to the crystal structure and unique magnetic nature of SPION. The core-shell system maintains the morphological features of SPIONs and the desired size range. Notably, Doxorubicin (DOX), an anticancer drug, was effectively entrapped into the polymeric shell of SPION@HP, showing a loading efficiency of 66.9 ± 2.7% and controlled release up to 120 h without any initial burst effect. Additionally, MTT assay revealed that DOX-loaded SPION@HP exerted great anticancer effect against HeLa cells and could be safely used. These results pave the way for the application of SPION@HP as an effective targeted delivery system for cancer treatment.

Iron Oxide Nanoparticles as Carriers for DOX and Magnetic Hyperthermia after Intratumoral Application into Breast Cancer in Mice: Impact and Future Perspectives

“…The fact, that DOX coupled to MNPs is basically able to interact with DNA is corroborated by: (1) the knowledge that upon degradation in lysosomes DOX is released from the MNPs, and as a free molecule DOX is able to migrate to the cell nucleus [ 36 ]; (2) previous investigations showing that DOX-loaded MNPs (e.g., electrostatic coupling; in absence of hyperthermia) exert a low intrinsic cytotoxicity [ 27 , 36 , 37 ]; and (3) the tumor reducing effect of our covalently coupled DOX-MNPs (4 µmol DOX/g Fe) is lower compared to that of the electrostatically coupled ones (40 µmol DOX/g Fe, [ 27 ]). All mentioned relationships indicate that the tumor reducing effect of our DOX-functionalized MNPs was due to a synergistic mechanism between DOX and hyperthermia, even though the comparably lower antitumor effect compared to the electrostatic MNP functionalization in former studies might well be due to a reduced number of DOX molecules per mg Fe and also due to the fact that covalent conjugation attenuates the release of DOX from the MNPs to some extent.…”

Applications of superparamagnetic iron oxide nanoparticles in drug and therapeutic delivery, and biotechnological advancements

“…Studies have shown that covalent binding of drugs can enable slow drug release at the targeted site. A functionalization that permits only adsorption can lead to premature drug release [ 33 , 46 , 80 ].…”

“…Depending on the type of emulsifier used, the coating can be hydrophilic or hydrophobic, but it is common to use hydrophilic polymers, such as PVA or PEG, for drug release studies [ 33 , 76 ] because the hydrophobic polymers are rapidly uptaken by macrophages [ 85 ]. SPIONs coated with a mixture of PVA and polyvinyl amine were shown to induce very active mitochondrial and endocytic processes in cells and to be highly toxic to cells due to the positive charge of the amine groups.…”

Synthesis and Characterization of Silica Coated Magnetic Iron Oxide Nanoparticles

“…5. From Figure 5, one can see that Fe 3 O 4 NPs, TSC@Fe 3 O 4 and SiO 2 coated Fe 3 O 4 NPs are all superparamagnetic because no hysteresis loop can be observed [13][14][15][16]. The saturation magnetization of Fe 3 O 4 NPs is 45.8 emu/g, which is higher than that of TSC@Fe 3 O 4 (~14.6 emu/g), SiO 2 coated Fe 3 O 4 NPs (~13.4 emu/g) due to the functionalization and the thick silica shell layer (~ 15 nm), respectively.…”