title: PEGylated polyplex micelles from triblock catiomers with spatially ordered layering of condensed pDNA and buffering units for enhanced intracellular gene delivery.
abstract: An A-B-C type triblock copolymer, tandemly aligning two types of polycations with different pKa values in a single polymer strand, was developed for the construction of novel polyplex micelles, satisfying a high DNA condensing ability as well as a proton buffering activity directed to elevating gene transfection. The micelle might feature the distinctive three-layered structure, where an inner polyplex layer of condensed pDNA with poly(l-lysine) (pKa approximately 9.4) as the C segment is successively wrapped with an intermediate layer of poly[(3-morpholinopropyl)aspartamide] (B segment) with a comparatively low pKa of approximately 6.2, to provide a buffering effect, and an outer PEG layer (A segment) as a biocompatible palisade.
authors.affiliation: Department of Materials Science and Engineering, Graduate School of Engineering, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-8656, Japan.
authors.forename: Shigeto
authors.initials: S
authors.lastname: Fukushima
authors.forename: Kanjiro
authors.initials: K
authors.lastname: Miyata
authors.forename: Nobuhiro
authors.initials: N
authors.lastname: Nishiyama
authors.forename: Naoki
authors.initials: N
authors.lastname: Kanayama
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Yamasaki
authors.forename: Kazunori
authors.initials: K
authors.lastname: Kataoka
mesh_terms: D001224:Aspartic Acid / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry*; D002021:Buffers; D002412:Cations; D002460:Cell Line; D018014:Gene Transfer Techniques; D005822:Genetic Vectors / Q000138:chemical synthesis / Q000737:chemistry; D006367:HeLa Cells; D006801:Humans; D007700:Kinetics; D008823:Micelles; D009025:Morpholines / Q000008:administration & dosage / Q000737:chemistry*; D010957:Plasmids / Q000008:administration & dosage / Q000737:chemistry* / Q000235:genetics; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000737:chemistry*; D011107:Polylysine / Q000008:administration & dosage / Q000737:chemistry*; D014162:Transfection
chemical_list: D002021:Buffers; D002412:Cations; D008823:Micelles; D009025:Morpholines; C499728:poly (3-morpholinopropyl) aspartamide; D011107:Polylysine; D001224:Aspartic Acid; D011092:Polyethylene Glycols