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.