title: Preparation of a Cyclic RGD: Modified Liposomal SiRNA Formulation for Use in Active Targeting to Tumor and Tumor Endothelial Cells.
abstract: The delivery of SiRNA is not only a challenging strategy for developing new remedies, but is also useful as an analytic tool for an in vivo phenotypic alteration by loss-of-function. Specifically, ligand-mediated SiRNA active targeting can be used to silence any gene in any organ of interest. In this chapter, we describe the preparation of an active targeting system to tumor endothelial cells (TECs) using liposomal SiRNA modified with cyclic RGD peptides. The procedure consists of essentially three steps: (1) the synthesis of a cyclic RGD peptide derivative, (2) SiRNA encapsulation into a liposomal delivery system, and (3) modification of liposomal SiRNA with a cyclic RGD derivative.
authors.affiliation: Faculty of Pharmaceutical Sciences, Hokkaido University, Sapporo, Hokkaido, 060-0812, Japan.
authors.forename: Yu
authors.initials: Y
authors.lastname: Sakurai
authors.affiliation: Faculty of Pharmaceutical Sciences, Hokkaido University, Sapporo, Hokkaido, 060-0812, Japan.
authors.forename: Tomoya
authors.initials: T
authors.lastname: Hada
authors.affiliation: Laboratory of Innovative Nanomedicine, Faculty of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo, Hokkaido, 060-0812, Japan. harasima@pharm.hokudai.ac.jp.
authors.forename: Hideyoshi
authors.initials: H
authors.lastname: Harashima
mesh_terms: D002626:Chemistry, Pharmaceutical; D042783:Endothelial Cells / Q000378:metabolism*; D008024:Ligands; D008055:Lipids / Q000737:chemistry; D008081:Liposomes / Q000737:chemistry*; D049329:Nanostructures / Q000737:chemistry; D009369:Neoplasms / Q000378:metabolism* / Q000473:pathology*; D010456:Peptides, Cyclic / Q000737:chemistry*; D034741:RNA, Small Interfering / Q000737:chemistry* / Q000378:metabolism
chemical_list: D008024:Ligands; D008055:Lipids; D008081:Liposomes; D010456:Peptides, Cyclic; D034741:RNA, Small Interfering; C507169:cyclic arginine-glycine-aspartic acid peptide
keywords: Active targeting; Liposomal delivery system; SiRNA; Tumor; Tumor endothelial cells