Novel polycationic phospholipid conjugates for gene carriers

Takehisa Dewa*, Yukari Ieda, Kazuyuki Morita, Kiyotaka Yoshida, Li Wang, Robert C. MacDonald, Kouji Iida, Keiji Yamashita, Naoto Oku, Mamoru Nango

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract

Three types of polycationic phospholipids conjugates were synthesized to develop a novel nonviral gene carrier. The conjugates composed of a polyamine portion: spermidine, spermine or polyethylenimine (PEI), and a phospholipid portion: dipalmitoylphosphatidic acid (DPPA) were synthesized via a synthetic intermediate, ethylbrominated DPPA. The polycationic lipids exhibited moderate transfection efficacy evaluated by β-galactosidase assay. These conjugates form a micelle-like assembly in aqueous solution, whose sizes are in the range of 90∼220 nm. The formation of the conjugate-DNA complex was observed by using atomic force microscopy (AFM). The AFM images revealed that the conjugate-bearing spermidine, which showed the most efficient transfection, enables one to form a compact complex (∼130 nm in width) with DNA, while the conjugate-bearing PEI, which showed a less efficient transfection, forms a large complex (∼200 nm) with DNA.

Original languageEnglish (US)
Pages (from-to)634-639
Number of pages6
JournalKobunshi Ronbunshu
Volume61
Issue number12
DOIs
StatePublished - Dec 2004

Keywords

  • AFM
  • Compaction
  • Gene transfer
  • Polyamine
  • Polycationic lipid

ASJC Scopus subject areas

  • Chemical Engineering (miscellaneous)
  • Materials Science (miscellaneous)
  • General Environmental Science
  • Polymers and Plastics

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