Phthalocyanines　are　promising　photosensitizers　for　photodynamic　therapy　(PDT),　but　the　inherent　tendency　of　aggregation　generally　leads　to　the　decrease　or　even　quenching　of　photoactivities.　To　address　this　issue　and　realize　the　desirable　photodynamic　therapeutic　effect　of　phthalocyanines,　herein,　we　report　a　folate-modified　phthalocyanine-based　liposomal　nanophotosensitizer　(PcN@Lip-FA),　which　can　be　prepared　through　a　facile　＇one-pot＇　method.　An　analogue　(PcN@Lip)　without　folate　was　also　prepared　as　a　negative　control.　The　liposomal　nanophotosnesitizers　greatly　prevented　the　aggregation　of　the　zinc(II)　phthalocyanine　(PcN)　and　showed　highly　efficient　photoactivities　(fluorescence　and　singlet　oxygen　generation)　in　aqueous　solutions,　although　the　free　PcN　is　severely　aggregated　and　its　photoactivities　are　nearly　quenched.　The　in　vitro　results　demonstrate　that　PcN@Lip-FA　can　be　taken　in　by　folate　receptor　(FR)-positive　HeLa　cells　through　FR-mediated　process,　and　exhibits　significantly　higher　cellular　uptake　and　photocytotoxicity　against　HeLa　cells　than　both　PcN@Lip　and　PcN,　but　for　FR-negative　MCF-7　cells,　PcN@Lip-FA　and　PcN@Lip　show　comparable　photocytotoxicity.　In　addition,　with　the　folate　vector,　PcN@Lip-FA　has　highly　efficient　tumor　targeting　and　PDT　effect　on　the　S180　rat　ascitic　tumor-bearing　mice　with　a　tumor　inhibition　rate　up　to　98.0%.　Therefore,　the　liposomal　nanophotosensitizer　PcN@Lip-FA　can　serve　as　a　promising　nanoplatform　for　cancer　diagnosis　and　targeted　PDT.　©　2020　Elsevier　Ltd