BSA-encapsulated cyclometalated iridium complexes as nano-photosensitizers for photodynamic therapy of tumor cells

Photodynamic therapy is a promising treatment method. The development of suitable photosensitizers can improve therapeutic efficacy. Herein, we report three iridium complexes (Ir1, Ir2, and Ir3), and encapsulate them within bovine serum albumin (BSA) to form nano-photosensitizers (Ir1@BSA, Ir2@BSA, and Ir3@BSA) for photodynamic therapy (PDT) of tumor cells. In the structures of Ir(iii) complexes, we use the pyrazine heterocycle as part of the C^N ligands and explore the effect of different ligands on the ability to generate singlet oxygen ((1)O(2)) by changing the conjugation length of the ligand and increasing the coplanarity of the ligand. Besides, the fabricated nano-photosensitizers are beneficial to improve water dispersibility and increase cellular uptake ability. Through studying photophysical properties, (1)O(2) generation capacity, and cellular uptake performance, the results show that Ir1@BSA has the best photodynamic therapeutic effect on 4T1 tumor cells. This study provides an effective research basis for the further design of new nano-photosensitizers.