Metwally, A. A. and Blagbrough, I. S., 2011. Self-assembled lipoplexes of short interfering RNA (siRNA) using spermine-based fatty acid amide guanidines: effect on gene silencing efficiency. Pharmaceutics, 3 (3), pp. 406-424.
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.
|Item Type ||Articles|
|Creators||Metwally, A. A.and Blagbrough, I. S.|
|Uncontrolled Keywords||self-assembly, lipoplexes, guanidine, gfp, sirna, fatty acids, spermine, gene silencing, nanoparticles|
|Departments||Faculty of Science > Pharmacy & Pharmacology|
|Publisher Statement||Pharmaceutics_2011_3_406-424_AAM_ISB.pdf: This is an Open Access article, provided under a Creative Commons Attribution Licence. The full citation for this article is: 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. DOI: http://dx.doi.org/10.3390/pharmaceutics3030406|
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