Bladder Cancer Photodynamic Therapeutic Agent with Off‐On Magnetic Resonance Imaging Enhancement

Abstract

Abstract Acting as an extracellular matrix protein receptor, α V β 3 integrin becomes an appealing target for photodynamic therapy of bladder cancer. Here, specific α V β 3 ‐integrin‐targeting porphyrinato‐gadolinium complexes (Gd‐PEG‐R n ) are demonstrated as off‐on theranostic agents, where R n are specific peptides. Among them, Gd‐PEG‐R 3 shows both impressive phototherapeutic index and robust in vivo magnetic resonance imaging (MRI) signal enhancement. Significant selectivity of Gd‐PEG‐R 3 is proven by its high α V β 3 integrin binding affinity in positive bladder cancer cells. All these findings support Gd‐PEG‐R 3 as a promising bi‐functional medical agent with both MRI contrasting ability and photodynamic therapeutic potential for curing bladder cancer.