Iron(III) Coordinated Theranostic Polyprodrug with Sequential Receptor-Mitochondria Dual Targeting and T 1 -Weighted Magnetic Resonance Imaging Potency for Effective and Precise Chemotherapy.

The sequential cancer cell receptor and mitochondria dual-targeting single delivery agent deliver chemotherapeutic drug effectively and precisely at the targeted site has become a promising strategy to enhance the drug efficacy and suppressions of cancer cell drug resistance prominence. Herein, required specialty molecules like a chemotherapeutic drug [camptothecin (CPT)], mitochondriotropic segment (triphenyl phosphonium cation) receptor targeting ligand (biotin), and magnetic resonance imaging (MRI)-contrast agent (iron-complex) were tethered to the polyprodrug, CP TP PG BN Fe , using the ring-opening metathesis polymerization technique for potential chemotherapy and simultaneous MRI-based diagnosis. This amphiphilic polyprodrug spontaneously aggregated into nanospheres and exhibited remarkable T 1 -weighted MRI proficiency. Detail in vitro cellular studies revealed unambiguous mitochondrial delivery of CPT, which eventually enhanced the chemotherapeutic efficacy of CP TP PG BN Fe . Therefore, MRI-tracking, receptor-mitochondria dual targeting, theranostic polyprodrug, and CP TP PG BN Fe opened the way for effective and precise chemotherapy, which would have the attractive potential for diagnosis and decisive dose determination in clinical implications.