Prostate cancer (PCa) is the second most prevalent cancer in males globally, impacting one out of every six males. However, the therapeutic effect of chemotherapy on PCa is restricted. To address this, we developed a tumor-targeted multifunctional liposomal platform (PTX-PS/Zn@Lip-Apt) for zinc-enhanced chemo-photodynamic therapy of PCa. Co-delivery of PTX and an aggregation-induced emission photosensitizer (TPEDPD) enables combined chemotherapy and photody-namic therapy. Zinc ions were loaded into liposomes to improve the chemosensitivity of PCa to chemodrugs. Then, the AS1411 aptamer was further modified onto the sur-face of the liposome to enhance its tumor targeting ability. Moreover, to improve the cellular uptake efficiency of the nanoparticles, the photochemical internalization (PCI) strategy was also employed. : In vitro experiments indicated that aptamer conjugation and PCI application enhanced the cellular uptake and cytotoxicity of PTX/PS-Zn@Lip-Apt. The zinc ion enhanced cytotoxicity could also be found. In vivo experiments demonstrated the good antitumor effect and biosafety of PTX/PS-Zn@Lip-Apt. : Our findings provide an important basis for innovatively applying zinc-enhanced combined chemo-photodynamic therapy in prostate cancer.