Nanosized　drug　delivery　systems　(NDDS)　with　photothermal　therapy　(PTT)　and　photodynamic　therapy　(PDT)　have　been　extensively　exploited　to　improve　the　therapeutic　performance　and　bio-safety　of　chemotherapeutic　drugs　in　cancer.　In　this　work,　a　carrier-free　nanodrug　was　developed　by　co-assembly　of　the　anti-cancer　agent　ursolic　acid　(UA),　an　asialoglycoprotein　receptor　(ASGPR),　which　can　recognize　the　target　molecule　lactobionic　acid　(LA),　and　the　near-infrared　(NIR)　probe　dye　indocyanine　green　(ICG)　to　form　UA-LA-ICG　NPs　by　a　simple　and　green　self-assembly　approach.　The　UA-LA-ICG　NPs　had　suitable　stability,　showed　controlled　release　profile　of　UA　drugs,　and　exhibited　preferable　temperature　response　(similar　to　59.4　degrees　C)　under　laser　irradiation　(808　nm,　1　W/cm(2)).　Compared　with　free　ICG,　the　UA-LA-ICG　NPs　significantly　enhanced　the　intracellular　ICG　uptake.　Upon　irradiation　of　the　NIR　laser,　co-assembled　nanodrugs　demonstrated　great　performance　as　a　reactive　oxygen　species　(ROS)　producer　and　exhibited　more　anti-proliferative　activities　on　ASGPR-overexpressing　HepG2　cells　than　ASGPR　low-expressing　HeLa　cells.　Meanwhile,　in　vivo　NIR　fluorescence　imaging　exhibited　that　the　co-assembled　nanodrugs　were　specifically　targeted　to　the　tumor　by　the　active　targeting　property　of　LA,　and　its　circulation　time　was　much　longer　than　that　of　free　ICG.　In　addition,　UA-LA-ICG　NPs　+　NIR　irradiation　treatment　displayed　enhanced　inhibitory　effect　on　tumor　growth　in　H22　tumor-bearing　mice.　Overall,　the　co-assembly　of　chemotherapeutic　agent　and　photosensitizer　by　the　self-assembly　approach　might　open　an　alternative　avenue　and　give　inspiration　to　fabricate　new　carrier-free　nanodrugs　for　cancer　imaging　and　chemo-photo　combination　therapy.　Statement　of　Significance　The　present　study　for　the　first　time　reported　carrier-free　nanoparticles　(NPs)　by　co-assembly　of　a　natural　product　ursolic　acid　(UA),　an　asialoglycoprotein　receptor　(ASGPR)-recognized　sugar　molecule　lactobionic　acid　(LA),　and　the　near-infrared　dye　indocyanine　green　(ICG)　through　a　simple　and　green　approach.　The　preparation　process　of　nanodrugs　is　simple,　rapid,　effective,　and　labor-saving.　The　co-assembled　nanodrugs　were　capable　of　stabilizing　the　ICG　molecules　and　specifically　targeting　to　the　tumor,　which　could　increase　the　tumor　accumulation　in　cancer　imaging　and　also　enhance　the　efficacy　of　chemophototherapy.　(C)　2018　Acta　Materialia　Inc.　Published　by　Elsevier　Ltd.　All　rights　reserved.