Carbon network-hosted porphyrin as a highly biocompatible nanophotosensitizer for enhanced photodynamic therapy.

Abstract

Photodynamic therapy (PDT) has the characteristics of being simple and non-invasive, and with on-demand light control. However, most photosensitizers exhibit strong hydrophobicity, low quantum yields in water and low tumor selectivity. In this study, carbon network-hosted porphyrins (CPs) with high biocompatibility and efficient singlet oxygen (1O2) generation were developed to reduce the biotoxicity of photosensitizers and avoid quenching caused by hydrophobic aggregation for enhanced PDT. The CPs were prepared by a simple solid-phase synthesis method using porphyrin, green non-toxic citric acid and urea as the raw materials. The CPs exhibited excellent water solubility and high biocompatibility. Even when the concentration reached 1.5 mg mL-1, cells still had good biological activity. By separately fixing the porphyrins in the carbon network, the CPs avoided aggregation-induced inactivation and had high generation efficiency of 1O2. Furthermore, in order to improve the PDT effect, the CPs were modified with the upper nuclear targeting peptide TAT (T-CPs), which was used to target the nucleus and generate 1O2in situ to directly destroy genetic material. The proposed strategy provides a simple and green path to prepare nanophotosensitizers with high biocompatibility and efficient 1O2 generation for PDT.