Self-assembled lipoplexes of short interfering RNA (siRNA) using spermine-based fatty acid amide guanidines: effect on gene silencing efficiency

Abdelkader A Metwally, Ian S Blagbrough

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Four guanidine derivatives of N4,N9-diacylated spermine have been designed, synthesized, and characterized. These guanidine-containing cationic lipids bound siRNA and formed nanoparticles. Two cationic lipids with C18 unsaturated chains, N1,N12-diamidino-N4,N9-dioleoylspermine and N1,N12-diamidino-N4-linoleoyl-N9-oleoylspermine, were more efficient in terms of GFP expression reduction compared to the other cationic lipids with shorter C12 (12:0) and very long C22 (22:1) chains. N1,N12-Diamidino-N4-linoleoyl-N9-oleoylspermine siRNA lipoplexes resulted in GFP reduction (26%) in the presence of serum, and cell viability (64%). These data are comparable to those obtained with TransIT TKO. Thus, cationic lipid guanidines based on N4,N9-diacylated spermines are good candidates for non-viral delivery of siRNA to HeLa cells using self-assembled lipoplexes.
Original languageEnglish
Pages (from-to)406-424
Number of pages19
Issue number3
Publication statusPublished - 2011



  • self-assembly
  • lipoplexes
  • guanidine
  • GFP
  • siRNA
  • fatty acids
  • spermine
  • gene silencing
  • nanoparticles

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