Design and construction of polymerized-chitosan coated Fe3O4 magnetic nanoparticles and its application for hydrophobic drug delivery

• Fe3O4 nanoparticles were modified with carboxymethyl-β-cyclodextrin.
• The grafting of CM-β-CD onto Fe3O4 nanoparticles enhanced the drug loading capacity.
• The nanocarrier displayed excellent loading efficiency and magnetic property.
• The drug release from the nanocarriers was diffusion and swelling controlled.
• The drug release profile fits well with the Korsmeyer–Peppas model.

In this study, a novel hydrogel, chitosan (CS) crosslinked carboxymethyl-β-cyclodextrin (CM-β-CD) polymer modified Fe3O4 magnetic nanoparticles was synthesized for delivering hydrophobic anticancer drug 5-fluorouracil (CS-CDpoly-MNPs). Carboxymethyl-β-cyclodextrin being grafted on the Fe3O4 nanoparticles (CDpoly-MNPs) contributed to an enhancement of adsorption capacities because of the inclusion abilities of its hydrophobic cavity with insoluble anticancer drugs through host–guest interactions. Experimental results indicated that the amounts of crosslinking agent and bonding times played a crucial role in determining morphology features of the hybrid nanocarriers. The nanocarriers exhibited a high loading efficiency (44.7 ± 1.8%) with a high saturation magnetization of 43.8 emu/g. UV–Vis spectroscopy results showed that anticancer drug 5-fluorouracil (5-Fu) could be successfully included into the cavities of the covalently linked CDpoly-MNPs. Moreover, the free carboxymethyl groups could enhance the bonding interactions between the covalently linked CDpoly-MNPs and anticancer drugs. In vitro release studies revealed that the release behaviors of CS-CDpoly-MNPs carriers were pH dependent and demonstrated a swelling and diffusion controlled release. A lower pH value led to swelling effect and electrostatic repulsion contributing to the protonation amine impact of NH3+, and thus resulted in a higher release rate of 5-Fu. The mechanism of 5-Fu encapsulated into the magnetic chitosan nanoparticles was tentatively proposed.

A novel nanocarrier, chitosan-coated magnetic drug carrier nanoparticle (CS-CDpoly-MNPs) is fabricated for the delivery of insoluble anticancer drug by grafting CM-β-CD onto the magnetite surface. The grafting of CM-dextrins onto the surface of Fe3O4 nanocrystal clusters can markedly increase the loading capacity of 5-Fu by virtue of CM-dextrins/5-Fu inclusion complex formation. The release of 5-Fu from nanocomposite carriers is pH dependent and displays different release efficiencies in various release media solutions.Figure optionsDownload as PowerPoint slide