title: Preparation of pH-sensitive liposomes retaining SOD mimic and their anticancer effect.
abstract: We prepared an anticancer drug based on a pH-sensitive liposome retaining Fe-porphyrin as an SOD mimic. The liposomes contained cationic/anionic lipid combinations and were composed of Fe-porphyrin, 1,2-dimyristoyl-sn-glycero-3-phosphatidylcholine, dimethylditetradecylammonium bromide, sodium oleate, and Tween-80. The Fe-porphyrin was released from the liposome at low pH, and the cytotoxicity for cancer cells by the liposome depended on the acidic environments of the endosomes in the cells. Furthermore, although the liposome exhibited an excellent anticancer effect on a gastric cancer cell line, the SOD activity of Fe-porphyrin was shown to have a significant influence on the cytotoxicity toward cancer cells. These findings suggest that the pH-sensitive liposome retaining the Fe-porphyrin as an SOD mimic promises to be a novel anticancer drug for endosomal escape.
authors.affiliation: Department of Applied Chemistry, Tokyo Metropolitan University, Hachioji, Tokyo 192-0397, Japan.
authors.forename: Kazue
authors.initials: K
authors.lastname: Hiraka
authors.forename: Mayuko
authors.initials: M
authors.lastname: Kanehisa
authors.forename: Miho
authors.initials: M
authors.lastname: Tamai
authors.forename: Shoichiro
authors.initials: S
authors.lastname: Asayama
authors.forename: Shoji
authors.initials: S
authors.lastname: Nagaoka
authors.forename: Kenichi
authors.initials: K
authors.lastname: Oyaizu
authors.forename: Makoto
authors.initials: M
authors.lastname: Yuasa
authors.forename: Hiroyoshi
authors.initials: H
authors.lastname: Kawakami
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000627:therapeutic use; D045744:Cell Line, Tumor; D016503:Drug Delivery Systems; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008081:Liposomes / Q000138:chemical synthesis*; D008665:Metalloporphyrins / Q000008:administration & dosage / Q000145:classification / Q000627:therapeutic use; D013274:Stomach Neoplasms / Q000188:drug therapy*; D013482:Superoxide Dismutase / Q000502:physiology*
chemical_list: D000970:Antineoplastic Agents; D008081:Liposomes; D008665:Metalloporphyrins; C015213:ferric porphine complex; D013482:Superoxide Dismutase