title: [Liposome modified with VIP-lipopeptide as a new drug delivery system].
abstract: We have designed a novel lipid analog (lipopeptide) that mimics the structural features of modified phospholipids. This lipopeptide is easily synthesized using a peptide synthesizer and has been shown to be useful for the modification of liposomes, which are used as an active targeted drug delivery system (DDS). Vasoactive intestinal peptide (VIP) has high homology with pituitary adenylate cyclase activating peptide (PACAP). There are three major PACAP receptors: PAC1R, VPAC1R, and VPAC2R. PAC1R has affinity only for PACAP, whereas VPAC1R and VPAC2R have the same affinity for both VIP and PACAP. In the present study, we synthesized several lipopeptides conjugated with VIP through different linkers and found that liposomes modified with these lipopeptides (VIP-Lips) selectively recognized the PACAP/VIP receptors. The anti-cancer activity of these VIP-Lips was evaluated by encapsulation of an antitumor drug, doxorubicin (DOX), into the modified liposomes (VIP-Lips-DOX) against the human osteosarcoma cell line, Saos-2, which highly expresses the VIP receptor. cAMP production was then measured to determine how well the VIP-Lips were able to recognize VPAC2R. The results clearly indicate that the proposed lipopeptide methodology holds promise as a DDS for cancer therapy.
authors.affiliation: School of Pharmaceutical Sciences, Toho University.
authors.forename: Toru
authors.initials: T
authors.lastname: Masaka
authors.forename: Yingpeng
authors.initials: Y
authors.lastname: Li
authors.forename: Sho
authors.initials: S
authors.lastname: Kawatobi
authors.forename: Yuki
authors.initials: Y
authors.lastname: Koide
authors.forename: Akira
authors.initials: A
authors.lastname: Takami
authors.forename: Kenji
authors.initials: K
authors.lastname: Yano
authors.forename: Ryosuke
authors.initials: R
authors.lastname: Imai
authors.forename: Nobuhiro
authors.initials: N
authors.lastname: Yagi
authors.forename: Hideharu
authors.initials: H
authors.lastname: Suzuki
authors.forename: Hidemasa
authors.initials: H
authors.lastname: Hikawa
authors.forename: Ichirou
authors.initials: I
authors.lastname: Tatsuno
authors.forename: Katsuhide
authors.initials: K
authors.lastname: Terada
authors.forename: Yusaku
authors.initials: Y
authors.lastname: Yokoyama
mesh_terms: D045744:Cell Line, Tumor; D002470:Cell Survival; D016503:Drug Delivery Systems; D006801:Humans; D008081:Liposomes / Q000737:chemistry; D014660:Vasoactive Intestinal Peptide / Q000737:chemistry*
chemical_list: D008081:Liposomes; D014660:Vasoactive Intestinal Peptide