Targeted and oxygen-enriched polymeric micelles for enhancing photodynamic therapy

Abstract Photodynamic therapy (PDT) has been emerged as an alternative therapeutic modality in treatment of several malignant tumors. However, the therapeutic efficacy of PDT is often limited by the solubility of photosensitizers, tumor hypoxia and lack of target specificity to cancer cells. In this study, we developed a folate-conjugated fluorinated polymeric micelle (PFFA) to deliver the hydrophobic photosensitizer (chlorin e6, Ce6) to overcome these limitations. The fluorinated micelles exhibit the low critical micelle concentration, good long-term stability, higher oxygen-carrying capacity and better singlet oxygen generation efficiency compared to non-fluorinated micelles, indicating the potential to improve the PDT efficacy in hypoxic conditions. Cytotoxicity of PDT effect and cellular uptake demonstrate the higher cell growth inhibition to HeLa cells upon irradiation attributed to the selective internalization of Ce6-loaded PFFA micelles (PFFA-Ce6). All results demonstrate the PFFA-Ce6 micelles with targeting function and oxygen-carrying capacity can serve as a promising drug delivery system for hydrophobic photosensitizers and improvement on PDT efficacy.