Abstract
Three different ionene polymers with varying quaternary ammonium moieties were used as a proof of concept for the formulation of antisense oligonucleotides, which are capable of inhibiting Renilla luciferase messenger ribonucleic acid (mRNA). Cationic vesicles, consisting of cationic polymer, antisense oligonucleotide (Luc) and non-ionic surfactant polysorbate 80, were investigated regarding their ζ potential, cytotoxicity and transfection efficiency. Deoxyribonucleic acid- (DNA) forming complexes in the presence of cationic vesicles were also investigated in terms of small-angle X-ray scattering (SAXS). The studied cationic vesicles showed very little, if any, toxicity against HeLa cells. Transfection abilities proved to vary strongly depending on the present quaternary ammonium moiety.
Highlights
The last decades have witnessed a growing interest in the use of synthetic oligonucleotides for the inhibition of gene expression [1] as an alternative to the classical small molecule drugs to treat diseases
The cryo-SEM analysis revealed spherical morphologies of the particles with similar average sizes (340 nm) than those achieved through the use of dynamic light scattering (DLS), as previously described. These results show the appropriateness of the use of C6-ionene polymer as a non-viral vehicle for nucleic acids
Cationic vesicles derived from ionene polymers with an alternating α,ω-tertiary diamine linker and the non-ionic surfactant polysorbate 80 were used to entrap oligonucleotide single strands which were complementary to Renilla luciferase messenger ribonucleic acid (mRNA)
Summary
The last decades have witnessed a growing interest in the use of synthetic oligonucleotides for the inhibition of gene expression [1] as an alternative to the classical small molecule drugs to treat diseases. Examples for such oligonucleotides are antisense oligonucleotides, short interfering RNAs (siRNAs) [2], aptamers [3], DNA/RNAzymes and antisense-induced exon skipping [4,5]. The first problem to solve is the high sensitivity of oligonucleotides towards degradation by serum nucleases. Several alternatives for viral transfection methods have been developed including formulations as a very fast and simple method [8]
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