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Pharmaceutics 2011, 3(3), 406-424; doi:10.3390/pharmaceutics3030406
Article

Self-Assembled Lipoplexes of Short Interfering RNA (siRNA) Using Spermine-Based Fatty Acid Amide Guanidines: Effect on Gene Silencing Efficiency

 and *
Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, UK
* Author to whom correspondence should be addressed.
Received: 13 May 2011 / Revised: 20 June 2011 / Accepted: 5 July 2011 / Published: 13 July 2011
(This article belongs to the Special Issue Gene Therapy)
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Abstract

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.
Keywords: fatty acids; gene silencing; GFP; guanidine; lipoplexes; nanoparticles; self-assembly; siRNA; spermine fatty acids; gene silencing; GFP; guanidine; lipoplexes; nanoparticles; self-assembly; siRNA; spermine
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Metwally, A.A.; Blagbrough, I.S. Self-Assembled Lipoplexes of Short Interfering RNA (siRNA) Using Spermine-Based Fatty Acid Amide Guanidines: Effect on Gene Silencing Efficiency. Pharmaceutics 2011, 3, 406-424.

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