Localization-dependent cell-killing effects of protoporphyrin (PPIX)-lipid micelles and liposomes in photodynamic therapy

Shoji Tachikawa, Shinichi Sato, Hisanao Hazama, Yasufumi Kaneda, Kunio Awazu, Hiroyuki Nakamura

Research output: Contribution to journalArticlepeer-review

17 Citations (Scopus)


The protoporphyron (PPIX)-lipid (PL-C17) liposomes were successfully prepared from the corresponding micelles by post-inserted method. Both the PL-C17 micelles and liposomes were distributed in plasma membrane and cytoplasm after incubation of the cells with PL-C17 liposomes for 1 h. They translocated from plasma membrane into a certain organelle in the cells after incubation in the photosensitizer-free medium. Higher photo-cytotoxicity was observed in the PL-C17 micelles and liposomes localized in plasma membrane in comparison with those localized in the cytoplasm under light irradiation. The LDH assay revealed that cytopathic damages of the plasma membrane were observed in the PL-C17 micelles and liposomes highly localized in plasma membrane. The fluorescent intensity of the calcein-encapsulating DOPC liposomes post-inserted with PL-C17 increased after light irradiation, suggesting that the membrane disruption is possibly caused by oxidation of membrane lipids with ROS generated from photosensitizers and affects the photo-cytotoxicity in PDT.

Original languageEnglish
Pages (from-to)7578-7584
Number of pages7
JournalBioorganic and Medicinal Chemistry
Issue number24
Publication statusPublished - 2015 Dec 15
Externally publishedYes


  • Drug delivery system (DDS)
  • Lipid
  • Liposome
  • Micelle
  • Photodynamic therapy (PDT)
  • Protoporphyrin IX (PPIX)
  • Reactive oxygen species (ROS)

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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