title: Iodinated photosensitizing chitosan: self-assembly into tumor-homing nanoparticles with enhanced singlet oxygen generation.
abstract: A novel iodinated chitosan-backboned conjugate (GC-I-Ce6) was designed and prepared to fabricate self-assembled biopolymeric nanoparticles with heavy atom-effected enhanced singlet oxygen generation as well as biological merits. The heavy atom-rich nature of the hydrophobic particle interior was characterized with X-ray absorption and the modified photophysical properties of a chemically embedded photosensitizer, chlorin e6 (Ce6). From the comparative spectroscopic studies as well as cellular and animal experiments, it has been shown that the self-assembled GC-I-Ce6 nanoparticles have enhanced capability of singlet oxygen generation by the intraparticle heavy-atom effect, along with high tumor targetability in vitro and in vivo thanks to the glycol chitosan-surfaced exterior with biocompatible, positively charged and tumor-homing characteristics. Actual efficacy improvement in the photodynamic therapy of a human breast cancer cell line (MDA-MB-231) demonstrates potential of our photophysically and pharmaceutically motivated hybrid bioconjugate approach for nanomedicine applications.
authors.affiliation: Center for Theragnosis, Korea Institute of Science and Technology, 39-1 Hawolgok-dong, Seongbuk-gu, Seoul 136-791, Korea.
authors.forename: Chang-Keun
authors.initials: CK
authors.lastname: Lim
authors.forename: Jiyoung
authors.initials: J
authors.lastname: Shin
authors.forename: Ick Chan
authors.initials: IC
authors.lastname: Kwon
authors.forename: Seo Young
authors.initials: SY
authors.lastname: Jeong
authors.forename: Sehoon
authors.initials: S
authors.lastname: Kim
mesh_terms: D000818:Animals; D001940:Breast / Q000187:drug effects / Q000473:pathology; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology; D045744:Cell Line, Tumor; D048271:Chitosan / Q000737:chemistry*; D002735:Chlorophyllides; D016503:Drug Delivery Systems; D005260:Female; D054879:Halogenation; D006367:HeLa Cells; D006801:Humans; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D053758:Nanoparticles / Q000737:chemistry*; D010778:Photochemotherapy / Q000379:methods; D017319:Photosensitizing Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D011166:Porphyrins / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D026082:Singlet Oxygen / Q000737:chemistry*
chemical_list: D002735:Chlorophyllides; D017319:Photosensitizing Agents; D011166:Porphyrins; C118638:glycol-chitosan; D026082:Singlet Oxygen; C062985:phytochlorin; D048271:Chitosan