Abstract Integrating multiple targets and hence bio-distribution effectively for papillary thyroid carcinoma (PTC) treatment remains a significant challenge, which can be addressed by using suitable nano-scale materials. Herein, iRGD-modified graphene oxide (GO) loaded 131I are developed for the specific treatment of PTC strengthened integrin targeting. Fine structural characteristics of GO and GO-iRGDs were characterized by fourier transform infrared spectroscopy (FT-IR), scanning electron microscope (SEC), Raman spectrum and X-ray photoelectron spectroscopy (XPS). The results showed that there were characteristic peaks and chemical bonds on GO and GO-iRGDs by FT-IR, the D-peak and G-peak of GO disappeared by Raman spectrum and C-N bond with iRGD of GO-iRGDs were strong by XPS. These 131I-GO-iRGDs and 131I-GOs were taken up by PTC cell (TPC-1, BCPAP, and IHH-4) through endocytosis after 48 h and 72 h in cell uptake test, especially the uptake rate of 131I-GO50-iRGD was the highest. The CCK-8 cytotoxicity test of 131I-GO-iRGDs and 131I-GOs showed that these nanoparticles toxicity were higher than that of Na131I and finally promoted PTC death. In vitro data verified the targeting mechanism of GO and 131I for PTC cell line is based on the relevant advantages of binding cell, followed by iRGD-endowed cell surface transport. The tailored design of GO-iRGDs validates a promising paradigm for radioisotope (131-iodine) delivery to combat PTC resistance and metastasis resulting from poor target access for effective combination therapy.
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