The　outcome　of　application　of　epidermal　growth　factor　receptor　tyrosine　kinase　inhibitors　(EGFR-TKIs)　in　patients　with　non-small-cell　lung　cancer　(NSCLC)　always　suffers　from　acquired　drug　resistance.　Its　combination　with　other　therapies　has　been　explored　with　promising　synergistic　results.　Photodynamic　therapy　(PDT)　is　an　established　treatment　modality　for　NSCLC,　but　the　low　tumor　selectivity　of　currently　available　photosensitizers　(PSs)　hampered　the　wide　clinical　application　of　PDT.　Here,　we　synthesized　erlotinib　modified　chitosan　(ECs)　by　click　coupling　and　developed　ECs/indocyanine　green　(ICG)　self-assembled　nanoparticles　(GECs)　for　combined　targeted　chemo-photodynamic　therapy.　GECs　showed　oval-shaped　particles　with　a　diameter　of　267.5　nm,　a　zeta　potential　of　-15.2　mV,　and　considerable　photostability.　In　vitro　release　experiment　showed　that　erlotinib　and　ICG　could　be　slowly　released　from　GECs　in　acidic　condition　with　lysozyme.　GECs　were　capable　of　generating　reactive　oxygen　species　(ROS)　for　PDT　under　near-infrared　laser　irradiation.　GECs　showed　synergistic　molecular　targeted　and　photodynamic　therapeutic　effects　in　inhibition　of　cellular　growth　and　induction　of　apoptosis　in　NSCLC　cells.　This　study　demonstrated　that　the　GECs　could　be　a　promising　platform　by　combination　of　targeted　chemo-photodynamic　therapy　for　NSCLC　treatment.