131I-labeled multifunctional dendrimers modified with BmK CT for targeted SPECT imaging and radiotherapy of gliomas

Abstract

Aim: The poly(amidoamine) dendrimers modified with Buthus martensii Karsch chlorotoxin (BmK CT) were developed as a 131I delivery system for glioma-targeted imaging and therapy. Materials & methods: Dendrimers before and after labeling 131I were synthetized and their physicochemical properties were tested. The targeting and therapeutic efficacy of 131I-G5.NHAc-HPAO-(PEG-BmK CT)-(mPEG) dendrimer against glioma was evaluated in vitro and in vivo. Results: All the dendrimers were stable under different conditions. BmK CT modification increased the cellular uptake of dendrimers in C6 glioma cells, but not in the normal RLE-6TN cells. 131I-G5.NHAc-HPAO-(PEG-BmK CT)-(mPEG) dendrimer was radiochemically pure and could be applied in glioma-targeting single-photon emission CT (SPECT) imaging and radiotherapy. Conclusion: 131I-G5.NHAc-HPAO-(PEG-BmK CT)-(mPEG) complex is a promising multifunctional nanoplatform for glioma-specific nuclear imaging and radiotherapy.