Radioiodine‐131‐Labeled Theranostic Nanoparticles for Transarterial Radioembolization and Chemoembolization Combination Therapy of VX2 Liver Tumor

Abstract In interventional treatment, materials are administered into the blood supply artery and directly delivered to tumors, offering proper scenarios for nanomedicine potential clinical applications. Transarterial chemoembolization (TACE) and transarterial radioembolization (TARE) are effective treatment methods for hepatocellular carcinoma (HCC), but postoperative residual tumor may result in intrahepatic recurrence and distant metastasis. The combination therapy of TACE and TARE based on multifunctional nanoparticles (NPs) is expected to overcome the drug resistance in hypoxic tumors and improve the therapeutic effect. Herein, BaGdF 5 NPs are synthesized and then coated with polydopamine (PDA), conjugated with the chemotherapeutic drug cis‐diamminedichloride platinum (CDDP), radio‐labeled with therapeutic radionuclide 131 I, yielding 131 I‐BaGdF 5 @PDA‐CDDP NPs. The in vitro anti‐cancer effects of 131 I‐BaGdF 5 @PDA‐CDDP NPs are confirmed using CCK‐8 and γ‐H2AX assays in Huh7 cells. Mixed with Lipiodol, 131 I‐BaGdF 5 @PDA‐CDDP NPs are injected into the hepatic artery via a microcatheter to realize the TACE and TARE combination therapy in a rabbit VX2 liver tumor model. The results indicate that glucose metabolism is clearly decreased based on 18 F‐FDG PET imaging and the apoptosis of tumor cells is increased. Furthermore, 131 I and BaGdF 5 NPs can be used for SPECT imaging and CT/MR imaging respectively, facilitating real‐time monitoring of the in vivo biodistribution of 131 I‐BaGdF 5 @PDA‐CDDP NPs.