title: Smart polymeric micelles as nanocarriers for oligonucleotides and siRNA delivery.
abstract: The development of in vivo delivery systems for oligonucleotides and siRNA is strongly desired to achieve their clinical applications. Recently, polyplex micelles, which are formed through an electrostatic interaction between nucleic acid compounds (DNA and RNA) and poly(ethylene glycol) (PEG)-polycation block copolymers, have received much attention due to their nanometric-scaled size and excellent biocompatibility. Here, three types of newly engineered block copolymers were developed to construct polyplex micelles useful for oligonucleotides and siRNA delivery: (1) PEG-polycation diblock copolymers possessing diamine side-chain with distinctive pKa for siRNA encapsulation into polyplex micelles with high endosomal escaping ability, (2) Lactosylated PEG-(oligonucleotide or siRNA) conjugate through acid-labile beta-thiopropionate linkage to construct pH-sensitive PIC micelles, and (3) PEG-poly(methacrylic acid) block copolymer for the construction of organic/inorganic hybrid nanoparticles encapsulating siRNA.
authors.affiliation: Department of Materials Engineering, Graduate School of Engineering, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo 113-8656, Japan.
authors.forename: Kazunori
authors.initials: K
authors.lastname: Kataoka
authors.forename: Keiji
authors.initials: K
authors.lastname: Itaka
authors.forename: Nobuhiro
authors.initials: N
authors.lastname: Nishiyama
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Yamasaki
authors.forename: Motoi
authors.initials: M
authors.lastname: Oishi
authors.forename: Yukio
authors.initials: Y
authors.lastname: Nagasaki
mesh_terms: D006863:Hydrogen-Ion Concentration; D008823:Micelles; D053758:Nanoparticles / Q000737:chemistry*; D016376:Oligonucleotides, Antisense / Q000008:administration & dosage*; D011092:Polyethylene Glycols / Q000737:chemistry*; D011109:Polymethacrylic Acids / Q000737:chemistry*; D011506:Proteins / Q000737:chemistry*; D034741:RNA, Small Interfering / Q000008:administration & dosage*
chemical_list: D008823:Micelles; D016376:Oligonucleotides, Antisense; D011109:Polymethacrylic Acids; D011506:Proteins; D034741:RNA, Small Interfering; C099679:poly(methacrylic acid-ethylene glycol); C520182:polyethylene glycol-poly(3-((3-aminopropyl)amino)aspartamide); D011092:Polyethylene Glycols