title: Enhanced cellular uptake of protoporphyrine IX/linolenic acid-conjugated spherical nanohybrids for photodynamic therapy.
abstract: Protoporphyrin IX (PpIX) has wide applications in photodynamic diagnosis and photodynamic therapy (PDT) in many human diseases. However, poor water solubility and cancer cell localization limit its direct application for PDT. We improved the water-solubility and cellular internalization of PpIX to enhance PDT efficacy by developing biocompatible PpIX/linolenic acid-conjugated polyhedral oligomeric silsesquioxane (PPLA) nanohybrids. The resulting PPLA nanohybrids exhibited a quasi-spherical shape with a size of <200nm. (1)H NMR analysis confirmed the synthesis of PPLA. The singlet oxygen formation of PPLA nanohybrids on laser irradiation was detected by photoluminescence emission. Fluorescence-activated cell sorting (FACS) analysis displayed higher cellular internalization of PPLA compared with free PpIX. In addition, PPLA nanohybrids exhibited significantly reduced dark-toxicity and a high phototoxicity mostly because of apoptotic cell death against human gastric cancer cells. These results imply that the PPLA nanohybrid system may be applicable in PDT.
authors.affiliation: Department of Biomedical Engineering, Catholic University of Daegu, Gyeongsan 712-702, Republic of Korea.
authors.forename: Hye-In
authors.initials: HI
authors.lastname: Lee
authors.affiliation: Department of Biomedical Engineering, Catholic University of Daegu, Gyeongsan 712-702, Republic of Korea. Electronic address: yjkim@cu.ac.kr.
authors.forename: Young-Jin
authors.initials: YJ
authors.lastname: Kim
mesh_terms: D017209:Apoptosis / Q000187:drug effects; D001692:Biological Transport; D045744:Cell Line, Tumor; D004847:Epithelial Cells / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D006801:Humans; D008027:Light; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D009336:Necrosis / Q000139:chemically induced; D017646:Organosilicon Compounds / Q000737:chemistry*; D010316:Particle Size; D010718:Phosphatidylserines / Q000378:metabolism; D010778:Photochemotherapy / Q000379:methods; D017319:Photosensitizing Agents / Q000737:chemistry / Q000494:pharmacology*; D011524:Protoporphyrins / Q000737:chemistry / Q000494:pharmacology*; D026082:Singlet Oxygen / Q000378:metabolism; D017962:alpha-Linolenic Acid / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D017646:Organosilicon Compounds; D010718:Phosphatidylserines; D017319:Photosensitizing Agents; D011524:Protoporphyrins; D017962:alpha-Linolenic Acid; D026082:Singlet Oxygen; C028025:protoporphyrin IX
keywords: Gastric cancer; Nanohybrid; Photodynamic therapy; Polyhedral oligomeric silsesquioxane; Protoporphyrin IX