Purpose:　Zinc　phthalocyanine　(ZnPc)　has　been　applied　widely　in　photodynamic　therapy　(PDT)　with　high　ROS-production　capacity　and　intense　absorption　in　the　near-infrared　region.　However,　weak　tumor　targeting　and　the　aggregation　tendency　of　ZnPc　seriously　affect　the　therapeutic　effect　of　PDT.　Therefore,　overcoming　the　aggregation　of　ZnPc　and　enhancing　its　antitumor　effect　were　the　purpose　of　this　study.　Methods:　In　this　study,　we　first　found　that　the　aggregation　behaviors　of　the　photosensitizer　ZnPc(TAP)　4　,　ZnPc　substituted　by　tertiary　amine　groups,　were　regulated　finely　by　pH　and　that　ZnPc(TAP)　4　could　be　disaggregated　gradually　as　the　pH　descended.　ZnPc(TAP)　4　and　human　serum　albumin　(HSA)　molecules　were　assembled　into　nanoparticles　(NPs)　for　tumor　targeting.　Meanwhile,　the　chemotherapy　drug　paclitaxel　(Ptx)　was　loaded　into　HSA　NPs　together　with　ZnPc(TAP)　4　for　dual　antitumor　effects.　HSA　NPs　loading　both　ZnPc(TAP)　4　and　Ptx　(NP–　ZnPc[TAP]　4　–Ptx)　were　characterized　by　particle　size　and　in　vitro　release.　Cytotoxicity,　subcellular　localization,　tumor　targeting,　and　anticancer　effect　in　vivo　were　investigated　respectively.　Results:　We　found　that　NP–ZnPc(TAP)　4　–Ptx　had　good　stability　with　qualifying　particle　size.　Interestingly,　ZnPc(TAP)　4　was　released　from　the　NPs　and　the　photodynamic　activity　enhanced　in　the　acidic　environment　of　tumor.　In　addition,　NP–ZnPc(TAP)　4　–Ptx　had　prominent　cytotoxicity　and　time-dependent　subcellular　localization　characteristics.　Through　a　three-dimensional　animal　imaging　system,　NP–ZnPc(TAP)　4　–Ptx　showed　much-enhanced　tumor　targeting　in　tumor-bearing　mice.　Above　all,　NP–ZnPc(TAP)　4　–Ptx　was　demonstrated　to　have　the　synergistic　anticancer　effect　of　PDT　and　chemotherapy.　Conclusion:　NP–ZnPc(TAP)　4　–Ptx　had　enhanced　tumor　targeting　for　the　pH-sensitive　property　of　ZnPc(TAP)　4　and　the　transport　function　of　HSA.　NP–ZnPc(TAP)　4　–Ptx　possessed　a　double-anticancer　effect　through　the　combination　of　ZnPc(TAP)　4　and　Ptx.　This　drug-delivery　system　may　also　be　used　to　carry　chemotherapy　drugs　other　than　Ptx　for　improving　antitumor　effects.　©　2018　Wang　et　al.