TY - JOUR
T1 - Self-assembled lipoplexes of short interfering RNA (siRNA) using spermine-based fatty acid amide guanidines: effect on gene silencing efficiency
AU - Metwally, Abdelkader A
AU - Blagbrough, Ian S
PY - 2011
Y1 - 2011
N2 - 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.
AB - 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.
KW - self-assembly
KW - lipoplexes
KW - guanidine
KW - GFP
KW - siRNA
KW - fatty acids
KW - spermine
KW - gene silencing
KW - nanoparticles
UR - http://www.scopus.com/inward/record.url?scp=80053034979&partnerID=8YFLogxK
UR - http://dx.doi.org/10.3390/pharmaceutics3030406
U2 - 10.3390/pharmaceutics3030406
DO - 10.3390/pharmaceutics3030406
M3 - Article
SN - 1999-4923
VL - 3
SP - 406
EP - 424
JO - Pharmaceutics
JF - Pharmaceutics
IS - 3
ER -