2D van der Waals System Integrated with Targeting Radio‐Diagnostic and Imaging Functions

Abstract The folate receptor (FR), overexpressed in various cancers, is a key target in cancer imaging, diagnosis, and treatment. Here, a dual‐function 2D van der Waals system is developed to accurately and sensitively diagnose cancer by targeting FR. The radioisotope‐labeled LDH (layered double hydroxide) nanoplate with folate (FA) as a targeting moiety and indocyanine green (ICG) as a fluorescence agent ( ⁶⁴ Cu‐LDH–ICG/FA), and without FA ( ⁶⁴ Cu‐LDH–ICG), are prepared via hydrothermal reaction for PET and NIRF imaging. The targeting efficacy of these nanoplates is evaluated in cell lines with varying FR expressions (A549, H460, KB, and HeLa). Specific uptake of ⁶⁴ Cu‐LDH–ICG/FA into cells correlated with FR expression, showing a positive relationship between radioactivity and fluorescence intensity. PET and NIRF imaging of tumor‐bearing mice injected with ⁶⁴ Cu‐LDH–ICG/FA indicate higher uptake in HeLa cells with high FR expression compared to A549 and KB cells with lower FR expression. This FR‐targeted dual‐imaging nanoplate exhibits excellent diagnostic potential for cancer, suggesting significant promise for cancer theranostics in clinical trials.