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Glioma is one of the most common malignant brain tumors in adults.Chlorotoxin(CTX)has been identified as a targeting ligand to cross the blood brain barrier(BBB)and specifically bind to glioma.Through different conjugation approaches,CTX can be conjugated onto iron oxide nanoparticles(NPs),quantum dots,or rare-earth upconversion NPs for targeted magnetic resonance or fluorescence imaging of glioma.Likewise,CTX-conjugated NPs can also be used as a carrier system to load radionuclides,anticancer drugs or therapeutic genes for targeted chemotherapy or gene therapy of glioma,respectively.Here we review the recent advances in CTX-targeted NPs for imaging and therapy of glioma.