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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 *
Received: 13 May 2011; in revised form: 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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

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.

AMA Style

Metwally AA, Blagbrough IS. Self-Assembled Lipoplexes of Short Interfering RNA (siRNA) Using Spermine-Based Fatty Acid Amide Guanidines: Effect on Gene Silencing Efficiency. Pharmaceutics. 2011; 3(3):406-424.

Chicago/Turabian Style

Metwally, Abdelkader A.; Blagbrough, Ian S. 2011. "Self-Assembled Lipoplexes of Short Interfering RNA (siRNA) Using Spermine-Based Fatty Acid Amide Guanidines: Effect on Gene Silencing Efficiency." Pharmaceutics 3, no. 3: 406-424.


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