Folate　(FA)　and　heptamethine　cyanine　(Cy7)-modified　chitosan　(CF7)　was　synthesized　by　click　chemistry　and　its　self-assembled　nanoparticles　(CF7Ns)　were　developed　for　tumor-specific　imaging　and　photodynamic　therapy.　The　characterization　spectrum　confirmed　CF7　had　a　good　FA　and　Cy7　conjugation　efficacy.　The　diameter　of　CF7Ns　measured　by　DLS　was　about　291.6　nm,　and　the　morphology　observed　with　AFM　showed　filamentous　clusters　of　particles.　The　results　of　targeting　ability　of　CF7Ns　demonstrated　enhanced　targeting　behaviors　of　CF7Ns　compared　with　non-FA-modified　nanoparticles　C7Ns　in　FA　receptor-positive　HeLa　cells.　The　cytotoxicity　and　cell　apoptosis　assay　showed　that　CF7Ns　under　near-infrared　light　irradiation　led　to　more　apoptotic　cell　death　in　HeLa　cells　to　improve　the　therapeutic　efficacy.　The　mechanisms　of　the　photodynamic　effects　of　CF7Ns　were　demonstrated　through　measurement　of　intracellular　reactive　oxygen　species　and　the　apoptosis-related　cytokines.　These　results　suggested　that　CF7Ns　are　promising　tumor　targeting　carriers　for　simultaneous　fluorescence　imaging　and　photodynamic　therapy.　©　2017　American　Chemical　Society.