Highly Efficient Photodynamic Therapy with Mitochondria‐Targeting Aggregation‐Induced Emission Photosensitizer for Retinoblastoma

Abstract Retinoblastoma (RB) is an aggressive eye cancer in infancy and childhood, lethal by metastasis if left untreated. Currently, the survival rate and the chance of saving vision depend on the severity of the disease. In this work, a highly efficient photodynamic ophthalmic therapy for RB is reported by employing an isoquinolinium‐based aggregation‐induced‐emission (AIE) photosensitizer (PS) TPE‐IQ‐2O for photodynamic inactivation (PDI). TPE‐IQ‐2O is an efficient mitochondria‐targeting photosensitizer as an efficient guided photodynamic therapy (PDT) agent against cancer cells. Maximizing cancer‐selectively damage to tumors with minimized side effects on normal tissue is essential for effective anticancer PDT and provides long‐lasting protection against metastasis. In addition, TPE‐IQ‐2O can effectively reduce the degree of tissue inflammation by inhibiting the expression of related inflammatory factors. TPE‐IQ‐2O also exhibits excellent biocompatibility with a neglectable hemolysis effect on mouse red blood cells and almost no killing effect on mammalian cells, which enables its potential applications in the treatment of RB.