Targeted　delivery　of　therapeutic　agents　is　of　particular　interest　in　the　field　of　cancer　treatment.　However,　there　is　an　urgent　need　for　developing　clinically　promising　targeting　approaches　that　can　be　readily　administered　in　a　green　manner.　Methods:　Five　phthalocyanine　derivatives　bearing　different　anionic　and　cationic　groups　were　designed　and　synthesized.　Then,　their　binding　affinity　with　albumin　were　studied　using　gel　assays,　optical　spectra　and　computational　simulation.　Finally,　in　vitro　and　in　vivo　fluorescence　imaging　and　photodynamic　therapy　(PDT)　evaluations　were　carried　out.　Results:　The　two　positively　charged　compounds　could　selectively　bind　to　albumin　dimer　over　albumin　monomer,　while　the　three　negatively　charged　phthalocyanines　could　bind　to　both　albumin　monomer　and　dimer.　Following　systemic　administration,　the　phthalocyanines　show　improved　tumor　accumulation　via　transport　by　natural　albumin.　PDT　evaluations　indicate　that　one　of　the　positively　charged　compounds,　ZnPcN4,　shows　outstanding　phototherapeutic　efficacy　against　tumors　in　preclinical　models.　Conclusion:　Our　findings　demonstrate　that　the　use　of　water-soluble　phthalocyanines　as　photosensitizers　and　in　vivo　albumin　as　a　natural　carrier　may　provide　a　green　and　efficient　approach　for　tumor-targeted　imaging　and　therapy.