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

Pharmaceutics

Abdelkader A. Metwally¹ 

[1] id="af1-pharmaceutics-03-00406">Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY,

关键词: fatty acids;    gene silencing;    GFP;    guanidine;    lipoplexes;    nanoparticles;    self-assembly;    siRNA;    spermine;   

DOI  :  10.3390/pharmaceutics3030406

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2011 by the authors; licensee MDPI, Basel, Switzerland.