Brachytherapy has been clinically used for the treatment of malignant solid
tumors. However, the classic therapeutic radioactive 125I seed must be surgically implanted directly into
tumors. To avoid the surgery and prevent irrational radioactive distribution, radioiodine-loaded nanomaterials are ever-developing for
brachytherapy. Hence, it is still a notable challenge to obtain an advanced material that simultaneously incorporates features of high radiolabeling rate, short labeling time, good radiolabeling stability, and long
tumor retention time. Covalent organic frameworks (COFs), which are crystalline
polymers with ordered pores, are widely applied in guest delivery of drugs based on their high porosity and modifiable skeleton. Herein, we developed a functionalized nanoscale PEG-COF-Ag material, which could rapidly capture radioiodine reaching a 94% radiolabeling yield in 30 s. In addition, more than 95% 125I was maintained after 24 h in PBS (
phosphate-buffered saline) as well as in serum and over 90% for nearly 1 week. PEG-COF-Ag-125I (125I-COF) demonstrated excellent
cancer cell killing performance in vitro, and further experiments in vivo revealed a long
tumor retention time and effective
tumor treatment during the
radiotherapy. The results indicate that radioiodine-labeled PEG-COF-Ag could be potentially applied in
brachytherapy with a promising
therapeutic effect.