We report the development of neurotoxin-mediated upconversion nanoprobes for tumor targeting and visualization in living animals. The nanoprobes were synthesized by preparing polyethylenimine-coated hexagonal-phase NaYF(4):Yb,Er/Ce nanoparticles and conjugating them with recombinant chlorotoxin, a typical peptide neurotoxin that could bind with high specificity to many types of cancer cells. Nanoprobes that specifically targeted glioma cells were visualized by laser scanning upconversion fluorescence microscopy. Good probe biocompatibility was displayed with cellular and animal toxicity determinations. Animal studies were performed using Balb-c nude mice injected intravenously with the nanoprobes. The obtained high-contrast images demonstrated highly specific tumor binding and direct tumor visualization with bright red fluorescence under 980-nm near-infrared irradiation. The high sensitivity and high specificity of the neurotoxin-mediated upconversion nanoprobes and the simplification of the required optical device for tumor visualization suggest an approach that may help improve the effectiveness of the diagnostic and therapeutic modalities available for tumor patients.
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