Abstract
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.
| Original language | English |
|---|---|
| Pages (from-to) | 406-424 |
| Number of pages | 19 |
| Journal | Pharmaceutics |
| Volume | 3 |
| Issue number | 3 |
| DOIs | |
| Publication status | Published - 2011 |
Keywords
- self-assembly
- lipoplexes
- guanidine
- GFP
- siRNA
- fatty acids
- spermine
- gene silencing
- nanoparticles
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