self-assembled lipoplexes of short interfering rna (sirna) using spermine-based fatty acid amide guanidines effect on gene silencing efficiency自组装lipoplexes短核rna)使用spermine-based脂肪酸酰胺胍对基因沉默效率的影响.pdfVIP
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self-assembled lipoplexes of short interfering rna (sirna) using spermine-based fatty acid amide guanidines effect on gene silencing efficiency自组装lipoplexes短核rna)使用spermine-based脂肪酸酰胺胍对基因沉默效率的影响
Pharmaceutics 2011, 3, 406-424; doi:10.3390/pharmaceutics3030406
OPEN ACCESS
pharmaceutics
ISSN 1999-4923
/journal/pharmaceutics
Article
Self-Assembled Lipoplexes of Short Interfering RNA (siRNA)
Using Spermine-Based Fatty Acid Amide Guanidines: Effect on
Gene Silencing Efficiency
Abdelkader A. Metwally and Ian S. Blagbrough *
Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, UK
Author to whom correspondence should be addressed; E-Mail: prsisb@bath.ac.uk;
Tel.: +44-1225-386795; Fax: +44-1225-386114.
Received: 13 May 2011; in revised form: 20 June 2011 / Accepted: 5 July 2011 /
Published: 13 July 2011
4 9
Abstract: Four guanidine derivatives of N ,N -diacylated spermine have been designed,
synthesized, and characterized. These guanidine-containing cationic lipids bound siRNA
1 12
and formed nanoparticles. Two cationic lipids with C18 unsaturated chains, N ,N -
diamidino-N4 9 1 12 4 9
,N -dioleoylspermine and N ,N -diamidino-N -linoleoyl-N -oleoylspermine,
were more efficient in terms of GFP expression reduction compared to the other cationic
1 12 4
lipids with shorter C12 (12:0) and very long C22 (22:1) chains. N
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