Self‐Folding Macromolecular Drug Carrier for Cancer Imaging and Therapy

Nano‐sized contrast agents (NCAs) hold potential for highly specific tumor contrast enhancement during magnetic resonance imaging. Given the quantity of contrast agents loaded into a single nano‐carrier and the anticipated relaxation effects, the current molecular design approaches its limits. In this study, a novel molecular mechanism to augment the relaxation of NCAs is introduced and demonstrated. NCA formation is driven by the intramolecular self‐folding of a single polymer chain that possesses systematically arranged hydrophilic and hydrophobic segments in water. Utilizing this self‐folding molecular design, the relaxivity value can be elevated with minimal loading of gadolinium complexes, enabling sharp tumor imaging. Furthermore, the study reveals that this NCA can selectively accumulate into tumor tissues, offering effective anti‐tumor results through gadolinium neutron capture therapy. The efficacy and versatility of this self‐folding molecular design underscore its promise for cancer diagnosis and treatment. The rare effect of amplifying the relaxation of contrast agents conjugated to a synthetic polymer induced by intramolecular self‐folding is reported. This self‐folding macromolecule loaded with gadolinium complexes can provide specific contrast enhancement of tumors during magnetic resonance imaging and an efficient anti‐tumor effect with neutron capture therapy.