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• W2108995198 abstract "Cationic liposomes are a useful in vitro but as yet unproven in vivo delivery system for oligonucleotides. An understanding of the mechanism of delivery mediated by cationic lipid/oligonucleotide complexes has been lacking. In this review, we describe recent results concerning several steps of the delivery process, including the formation of complexes, the intracellular distribution of the oligonucleotide and the lipid, as well as the uptake pathway and site of intracellular release. Cationic liposomes form a polyelectrolyte complex with the oligonucleotides, protect them from nuclease degradation, enhance their cellular uptake and improve the oligonucleotide potency. In the majority of cell types studied, cationic lipids deliver oligonucleotides into the cell predominately via an endocytotic pathway rather then by fusion with the plasma membrane. We propose that the oligonucleotide is released from the complex when anionic lipids from the cytoplasmic facing lipid monolayer of the cell flip into contact with the complex, the anionic lipids then laterally diffuse into the complex and form a charged neutralized ion-pair with the cationic lipids. This leads to displacement of the oligonucleotide from the cationic lipid and its release into the cytoplasm. In most cell types this occurs after endocytosis of the complex rather than after fusion of the complex directly with the plasma membrane. These new concepts of oligonucleotide release in cells provide a useful starting point for the rationale improvement of this nucleic acid delivery system." @default.
• W2108995198 created "2016-06-24" @default.
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• W2108995198 date "1997-01-01" @default.
• W2108995198 modified "2023-09-25" @default.
• W2108995198 title "Cationic Liposomes as an Oligonucleotide Carrier: Mechanism of Action" @default.
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• W2108995198 doi "https://doi.org/10.3109/08982109709035480" @default.
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