Design, synthesis, and in vivo evaluation of GO-SWL-Ahx-K-SWL

Abstract

In order to acquire both expanded binding ability with the EphA2 receptor and superior drug delivery capacity, we designed and synthesized the modified GO-SWL-Ahx-K-SWL conjugate as a potential targeted therapeutic drug for non-small cell lung cancer (NSCLC). Various characterization methods have confirmed that the conjugate is consistent with the theoretical peptide. The cytotoxicity test results showed that the conjugate was slightly more toxic to A549 cells than in 3 T3 cells, and the toxicity increased in a concentration-dependent manner. Single photon emission computed tomography/computed tomography (SPECT/CT) fusion imaging was performed to evaluate the conjugate binding to EphA2 receptor in vivo. The images showed obvious radioactive concentration in tumor tissues and significantly higher ratios of the tumor and muscle in the ¹²⁵I-GO-SWL-Ahx-K-SWL group (10.78) than in the ¹²⁵I-SWL-Ahx-K-SWL group (5.21) at all three time points (P < 0.01).

Keywords: EphA2; Graphene oxide; Non-small cell lung cancer; SWL; Targeted therapy.