Preparation, characterization of 2-deoxy-D-glucose functionalized dimercaptosuccinic acid-coated maghemite nanoparticles for targeting tumor cells.

Purpose: To report a modified preparation and to systematically study the structure, magnetic and other properties of γ-Fe(2)O(3)-DMSA-DG NPs (2-deoxy-D-glucose (2-DG) conjugated meso-2,3-dimercaptosuccinic acid coated γ-Fe(2)O(3) nanoparticles) and test its ability to improve Hela tumor cells targeting in vitro compared to the γ-Fe(2)O(3)-DMSA NPs.

Methods: The conjugation of 2-DG on the surface of γ-Fe(2)O(3)-DMSA NPs was performed by esterification reaction and characterized. Acute toxicity was evaluated using MTT assay. Cellular uptake was investigated by Prussian blue staining and UV colorimetric assay.

Results: DG was successfully functionalized onto the surface of γ-Fe(2)O(3)-DMSA NPs; binding efficiency was ~60%. The mean diameter of single core of γ-Fe(2)O(3)-DMSA-DG NPs was 10 nm. Particle size and polydispersity index of its aggregates were 156.2 nm and 0.162, respectively. 2-DG-conjugated nanoparticles caused little cytotoxic effects on Hela cells at the concentration range of 0-600 μg/mL. When 2-DG-conjuated and non-conjugated nanoparticles were incubated with Hela cells for 4, 8 and 12 h, the 2-DG-conjugated nanoparticle showed significant amount of uptake in cells compared to their non-targeted counterparts.

Conclusion: γ-Fe(2)O(3)-DMSA-DG NPs could be developed as a tumor-targeted probe for cervical cancer imaging and therapy.