Self-Assembled PSMA-Targeted Nanoparticles Enhanced Photodynamic Therapy in Prostate Cancer

Prostate cancer greatly threatens human health. Many treatment strategies including surgery and radiotherapy are applied to treat prostate cancer. However, these treatment strategies will bring great side effects. Herein, we developed a functionalized Prostate‐Specific Membrane Antigen‐Chlorin e6 (PSMA‐Ce6) NPs to enhance photodynamic therapy to reduce the side effects of prostate cancer treatments. We linked the hydrophobic photosensitizer Ce6 with the small hydrophilic molecule PSMA ligand through a covalent bond to form a functionalized PSMA‐Ce6. In aqueous phase, the PSMA‐Ce6 self‐assembled into nanoparticles with a hydrophobic core and a hydrophilic shell, which significantly enhanced the accumulation of PSMA‐Ce6 in the tumor. The molecularly targeted drug PSMA inhibitor can not only specifically inhibit PSMA but also increase the accumulation of the photosensitizer Ce6 in the tumor and achieve a completed tumor ablation under the near infrared (NIR) irradiation. PSMA‐Ce6 NPs have great potential for translation into clinical applications.