title: Incorporation of Porphyrin to π-Conjugated Backbone for Polymer-Dot-Sensitized Photodynamic Therapy.
abstract: The photosensitizers used in photodynamic therapy are mainly based on porphyrin derivatives. However, clinical applications encounter several limitations regarding photosensitizers such as their low absorption coefficients, poor water-solubility, and leaching from delivery carriers. Here, we describe covalent incorporation of porphyrin in conjugated polymer backbone for development of efficient polymer-dot photosensitizer. Spectroscopic characterizations revealed that the light-harvesting polymer dominantly transfer the excitation energy to the porphyrin unit, yielding efficient singlet oxygen generation for photodynamic therapy. The polymer dots (Pdots) also possess excellent stability that overcomes the photosensitizer leaching problem as encountered in other nanoparticle carriers. In vitro cytotoxicity and photodynamic efficacy of the Pdots were evaluated in MCF-7 cells by in vitro assay, indicating that the Pdots can efficiently damage cancer cells. In vivo photodynamic therapy by using the Pdots was further investigated with xenograft tumors in Balb/c nude mice, which show that the tumors were significantly inhibited or eradicated in certain cases. The high-yield singlet oxygen generation and excellent stability of porphyrin-incorporated Pdots are promising for photodynamic treatment of malignant tumors.
authors.affiliation: State Key Laboratory on Integrated Optoelectronics, College of Electronic Science and Engineering, Jilin University , Changchun, Jilin 130012, China.
authors.forename: Kaiwen
authors.initials: K
authors.lastname: Chang
authors.affiliation: Department of Gastroenterology, The First Hospital of Jilin University , Changchun, Jilin 130021, China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Tang
authors.affiliation: State Key Laboratory on Integrated Optoelectronics, College of Electronic Science and Engineering, Jilin University , Changchun, Jilin 130012, China.
authors.forename: Xiaofeng
authors.initials: X
authors.lastname: Fang
authors.affiliation: State Key Laboratory on Integrated Optoelectronics, College of Electronic Science and Engineering, Jilin University , Changchun, Jilin 130012, China.
authors.forename: Shengyan
authors.initials: S
authors.lastname: Yin
authors.affiliation: Department of Gastroenterology, The First Hospital of Jilin University , Changchun, Jilin 130021, China.
authors.forename: Hong
authors.initials: H
authors.lastname: Xu
authors.affiliation: State Key Laboratory on Integrated Optoelectronics, College of Electronic Science and Engineering, Jilin University , Changchun, Jilin 130012, China.
authors.forename: Changfeng
authors.initials: C
authors.lastname: Wu
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000473:pathology; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D005260:Female; D006801:Humans; D008027:Light; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000008:administration & dosage* / Q000737:chemistry; D011108:Polymers / Q000494:pharmacology*; D011166:Porphyrins / Q000737:chemistry*; D026082:Singlet Oxygen; D014407:Tumor Cells, Cultured; D023041:Xenograft Model Antitumor Assays
chemical_list: D004337:Drug Carriers; D017319:Photosensitizing Agents; D011108:Polymers; D011166:Porphyrins; D026082:Singlet Oxygen