Two arms hydrophilic photosensitizer conjugates with vitamin B for cancer‐selective photodynamic therapy

Cancer‐selective internalization has a great potential for reducing the side effect of photodynamic therapy. Recently, various cancer‐targeted delivery carriers have provided enhanced cancer targeting efficiency. Despite significant advancements in cancer‐targeted carriers, side effects are still present because of non‐selective cellular uptake that occurs in the heterogeneous cancer environment. In this paper, we designed two types of cancer‐selectable two arm hydrophilic photosensitizer (CTAHP2K and CTAHP4K) with silicon‐tetrapyrazinoporphyrazines (ST), polyethylene glycol and the cancer‐specific ligand for cancer‐selective theranostics. The synthesized CTAHP4K exhibits a folate receptor‐mediated cancer‐selective cellular uptake and induces cancer‐selective death. The folate receptor‐mediated cancer‐selective internalization of CTAHP4K was confirmed by competitive interaction with vitamin B in MDA‐MB‐231 human breast carcinoma. The cancer‐selective cytotoxicity of CTAHP4K was confirmed using a 670‐nm laser to irradiate Chang Liver cells and MDA‐MB‐231 cells. Copyright © 2016 John Wiley & Sons, Ltd.