Direct Labeling of Gold Nanoparticles with Iodine-131 for Tumor Radionuclide Therapy

利用碘-131直接标记金纳米粒子进行肿瘤放射性核素治疗

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Abstract

PURPOSE: Gold nanoparticles (Au NPs) are widely used as versatile templates to develop multifunctional nanosystems for disease diagnosis and treatment. Iodine can bind to gold via chemisorption, making this a simple method for labeling Au NPs with radioactive iodine. However, the evaluation of tumor radionuclide therapy is insufficient. In this study, we investigated the feasibility of (131)I-adsorbed Au NPs as novel nanoprobes for tumor radionuclide therapy. MATERIALS AND METHODS: Radiolabeling was performed by mixing Au NPs and (131)I, and the radiochemical purity (RCP) and in vitro stability of (131)I-adsorbed Au NPs were analyzed under different conditions, including various temperatures, pH values, and (131)I concentrations. The tumor accumulation and therapeutic potential of (131)I-adsorbed Au NPs were assessed using a subcutaneous tumor model after intratumoral injection. RESULTS: The data showed that the chemisorption of the Au NPs onto (131)I was instant, specific, and quantitative. The (131)I-adsorbed Au NPs exhibited high in vitro stability in different media, distinct inhibitory effects on tumor cells in vitro, good retention ability, and therapeutic effects after intratumoral injection into tumor-bearing mice in vivo. CONCLUSION: Our work demonstrates that chemisorption of Au NPs and radioiodine has great potential as a strategy for constructing various nanosystems for theranostic applications.

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