I-124 Labeled Rhein-coated gold nanoparticles for targeted breast cancer

Abstract

Rhein, an anthraquinone derivative, and gold nanoparticles have demonstrated significant potential in facilitating diagnostic applications and for possible theranostic use in breast cancer research. Rhein is known to interact with estrogen-α (ERα), which is relevant in ERα-positive breast cancer models. In addition, gold nanoparticles, when used as nanocarriers, may support imaging performance and delivery, although therapeutic effects require further validation. This study outlines the preparation of [¹²⁴I]rhein-gold for position emission tomography (PET) imaging in an ERα-positive breast cancer mouse model. The radiochemical yield of [¹²⁴I]RCGs was 65% ± 8.2%, with a radiochemical purity of >98%. In the evaluation of cellular uptake, a high uptake rate exceeding 25% was observed within 15 minutes. Corresponding results indicated a significantly elevated initial uptake rate, with a standardized uptake value mean (SUV_mean) greater than 6 in small animal PET imaging. This study demonstrated the synthesis and biological evaluation of [¹²⁴I]RCGs. [¹²⁴I]RCGs showed high cellular uptake in a time-dependent manner. PET images of [¹²⁴I]RCGs confirmed preferential uptake in ERα-positive MCF-7 tumors from 15 min to 240 min. These results suggest that [¹²⁴I]RCGs are promising radiopharmaceuticals, demonstrating potential as experimental PET imaging agents associated with ERα-positive breast cancer, while targeting should be considered implicit without blocking or control data.