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Pharmaceutics 2011, 3(2), 125-140; doi:10.3390/pharmaceutics3020125
Article

Efficient Gene Silencing by Self-Assembled Complexes of siRNA and Symmetrical Fatty Acid Amides of Spermine

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Received: 28 January 2011; in revised form: 11 March 2011 / Accepted: 22 March 2011 / Published: 25 March 2011
(This article belongs to the Special Issue Delivery and Genomics of Large Molecules)
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Abstract: Gene silencing by siRNA (synthetic dsRNA of 21-25 nucleotides) is a well established biological tool in gene expression studies and has a promising therapeutic potential for difficult-to-treat diseases. Five fatty acids of various chain length and oxidation state (C12:0, C18:0, C18:1, C18:2, C22:1) were conjugated to the naturally occurring polyamine, spermine, and evaluated for siRNA delivery and gene knock-down. siRNA delivery could not be related directly to gene silencing efficiency as N4,N9-dierucoyl spermine resulted in higher siRNA delivery compared to N4,N9-dioleoyl spermine. GFP silencing in HeLa cells showed that the unsaturated fatty acid amides are more efficient than saturated fatty acid amides, with N4,N9-dioleoyl spermine resulting in the most efficient gene silencing in the presence of serum. The alamarBlue cell viability assay showed that fatty acid amides of spermine have good viability (75%–85% compared to control) except N4,N9-dilauroyl spermine which resulted in low cell viability. These results prove that unsaturated fatty acid amides of spermine are efficient, non-toxic, non-viral vectors for siRNA mediated gene silencing.
Keywords: fatty acids; gene silencing; GFP; lipoplexes; self-assembly; siRNA; spermine fatty acids; gene silencing; GFP; lipoplexes; 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.; Pourzand, C.; Blagbrough, I.S. Efficient Gene Silencing by Self-Assembled Complexes of siRNA and Symmetrical Fatty Acid Amides of Spermine. Pharmaceutics 2011, 3, 125-140.

AMA Style

Metwally AA, Pourzand C, Blagbrough IS. Efficient Gene Silencing by Self-Assembled Complexes of siRNA and Symmetrical Fatty Acid Amides of Spermine. Pharmaceutics. 2011; 3(2):125-140.

Chicago/Turabian Style

Metwally, Abdelkader A.; Pourzand, Charareh; Blagbrough, Ian S. 2011. "Efficient Gene Silencing by Self-Assembled Complexes of siRNA and Symmetrical Fatty Acid Amides of Spermine." Pharmaceutics 3, no. 2: 125-140.



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