ArticlePharmaceutical research2009
Very long chain N4, N9 -diacyl spermines: non-viral lipopolyamine vectors for efficient plasmid DNA and siRNA delivery.
Article in Pharmaceutical research, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 18 citations in OpenAlex.
- Lipids and Lipid Derivatives for RNA Delivery.Chemical reviews · 2021Review
- Quantitative silencing of EGFP reporter gene by self-assembled siRNA lipoplexes of LinOS and cholesterol.Molecular pharmaceutics · 2012Article
- Biodegradation, biocompatibility, and drug delivery in poly(ω-pentadecalactone-co-p-dioxanone) copolyesters.Biomaterials · 2011Article
- Self-Assembled Lipoplexes of Short Interfering RNA (siRNA) Using Spermine-Based Fatty Acid Amide Guanidines: Effect on Gene Silencing Efficiency.Pharmaceutics · 2011Article
- Efficient Gene Silencing by Self-Assembled Complexes of siRNA and Symmetrical Fatty Acid Amides of Spermine.Pharmaceutics · 2011Article
- N1,N12-Diacyl spermines: SAR studies on non-viral lipopolyamine vectors for plasmid DNA and siRNA formulation.Pharmaceutical research · 2010Article
- Design and synthesis of N4,N9-disubstituted spermines for non-viral siRNA delivery--structure-activity relationship studies of siFection efficiency versus toxicity.Pharmaceutical research · 2009Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo study the effect of increasing the chain length over C-18 and varying the oxidation level in synthesized N4, N9-diacyl spermines on DNA and siRNA formulation, and then to compare their transfection efficiency in cell lines
methodsThe five novel very long chain N4, N9-diacyl polyamines: N4, N9-[diarachidoyl, diarachidonoyl, dieicosenoyl, dierucoyl and dinervonoyl]-1,12-diamino-4,9-diazadodecane were synthesized. The abilities of these novel compounds to condense DNA and to form nanoparticles were studied using ethidium bromide fluorescence quenching and nanoparticle characterization techniques. Transfection efficiency was studied in FEK4 primary skin cells and in an immortalized cancer cell line (HtTA), and compared with the non-liposomal transfection formulation Lipogen, N4, N9-dioleoyl-1,12-diamino-4,9-diazadodecane. Also, the abilities of these compounds to condense siRNA and to form nanoparticles were studied using a RiboGreen intercalation assay and their abilities to deliver siRNA into cells were studied in FEK4 and HtTA cells using fluorescein-labelled Label IT(R) RNAi Delivery Control, a sequenced 21-mer from Mirus.
resultsWe show efficient pEGFP and siRNA formulation and delivery to primary skin and cancer cell lines.
conclusionsAdding two C20 or C22 chains, both mono-cis-unsaturated, N4, N9-dieicosenoyl spermine and N4, N9-dierucoyl spermine, gave efficient siRNA delivery vectors, even in the presence of serum, comparable to TransIT-TKO and with excellent cell viability.
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