Ultrasmall c(RGDyK)-Coated Fe₃O₄ Nanoparticles and Their Specific Targeting to Integrin α_vβ₃-Rich Tumor Cells

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Abstract

We report a direct synthesis of ultrasmall c(RGDyK) peptide-coated Fe₃O₄ NPs (<10 nm in hydrodynamic diameter) and demonstrate their in vivo tumor-specific targeting capability. The Fe₃O₄ NPs are synthesized by thermal decomposition of iron pentacarbonyl in the presence of 4-methylcatechol (4-MC), and the peptide is coupled to the nanoparticles through 4-MC via Mannich reaction. The c(RGDyK)-MC-Fe₃O₄ NPs have an overall diameter of 8.4 nm and are stable in physiological conditions. When administrated intravenously, these c(RGDyK)-MC-Fe₃O₄ NPs accumulate preferentially in the integrin α_vβ₃-rich tumor area, which are readily tracked by MRI.

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