Phthalocyanines　are　potentially　promising　photosensitizers　(PSs)　for　photodynamic　therapy　(PDT),　but　the　inherent　defects　such　as　aggregation-caused　quenching　effects　and　non-specific　toxicity　severely　hinder　their　further　application　in　PDT.　Herein,　we　synthesized　two　zinc(II)　phthalocyanines　(PcSA　and　PcOA)　monosubstituted　with　a　sulphonate　group　in　the　alpha　position　with　＂O　bridge＂　and　＂S　bridge＂　as　bonds　and　prepared　a　liposomal　nanophotosensitizer　(PcSA@Lip)　by　thin-film　hydration　method　to　regulate　the　aggregation　of　PcSA　in　the　aqueous　solution　and　enhance　its　tumor　targeting　ability.　PcSA@Lip　exhibited　highly　efficient　production　of　superoxide　radical　(O-2(center　dot-))　and　singlet　oxygen　(O-1(2))　in　water　under　light　irradiation,　which　were　2.6-fold　and　15.4-fold　higher　than　those　of　free　PcSA,　respectively.　Furthermore,　PcSA@Lip　was　able　to　accumulate　selectively　in　tumors　after　intravenous　injection　with　the　fluorescence　intensity　ratio　of　tumors　to　livers　was　4.1:1.　The　significant　tumor　inhibition　effects　resulted　in　a　98%　tumor　inhibition　rate　after　PcSA@Lip　was　injected　intravenously　at　an　ultra-low　PcSA@Lip　dose　(0.8　nmol　g(-1)　PcSA)　and　light　dose　(30　J　cm(-2)).　Therefore,　the　liposomal　PcSA@Lip　is　a　prospective　nanophotosensitizer　possessing　hybrid　type　I　and　type　II　photoreactions　with　efficient　photodynamic　anticancer　effects.