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 (c) 2016 John Wiley & Sons, Ltd.