Cyclodextrins　(CDs),　as　pharmaceutical　excipients　with　excellent　biocompatibility,　non-immunogenicity,　and　low　toxicity　in　vivo,　are　widely　used　to　carry　drugs　by　forming　inclusion　complexes　for　improving　the　solubility　and　stability　of　drugs.　However,　the　limited　space　of　CDs＇　lipophilic　central　cavity　affects　the　loading　of　many　drugs,　especially　with　larger　molecules.　In　this　study,　β-CDs　were　modified　by　acetonization　to　improve　the　affinity　for　the　chemotherapy　drug　doxorubicin　(DOX),　and　doxorubicin-adsorbing　acetalated　β-CDs　(Ac-CD:DOX)　self-assembled　to　nanoparticles,　followed　by　coating　with　the　amphiphilic　zinc　phthalocyanine　photosensitizer　ZnPc-(PEG)5　for　antitumor　therapy.　The　final　product　ZnPc-(PEG)5:Ac-CD:DOX　was　demonstrated　to　have　excellent　stability　and　pH-sensitive　drug　release　characteristics.　The　cell　viability　and　apoptosis　assay　showed　synergistic　cytotoxic　effects　of　chemotherapy　and　phototherapy.　The　mechanism　of　cytotoxicity　was　analyzed　in　terms　of　intracellular　reactive　oxygen　species,　mitochondrial　membrane　potential,　and　subcellular　localization.　More　importantly,　in　vivo　experiments　indicated　that　ZnPc-(PEG)5:Ac-CD:DOX　possessed　significant　tumor　targeting,　prominent　antitumor　activity,　and　less　side　effects.　Our　strategy　expands　the　application　of　CDs　as　drug　carriers　and　provides　new　insights　into　the　development　of　CD　chemistry.　©