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https://www.ncbi.nlm.nih.gov/pubmed/19530907
However, the harsh biological milieu of the acidic stomach and enzyme-rich gastrointestinal tract make efficient delivery of oligonucleotides and siRNA via the oral route difficult. Nonetheless, the first studies on the oral delivery of siRNA in animals and antisense oligonucleotides in humans suggest that significant oral delivery of these nucleic acids can be achieved across the gut wall.Author: Saghir Akhtar
https://www.tandfonline.com/doi/abs/10.1080/10611860903057674
Apr 21, 2009 · However, the harsh biological milieu of the acidic stomach and enzyme-rich gastrointestinal tract make efficient delivery of oligonucleotides and siRNA via the oral route difficult. Nonetheless, the first studies on the oral delivery of siRNA in animals and antisense oligonucleotides in humans suggest that significant oral delivery of these ...Author: Saghir Akhtar
https://www.researchgate.net/publication/26296131_Oral_delivery_of_siRNA_and_antisense_oligonucleotides
Oral delivery of siRNA and antisense oligonucleotides. Inhibition of gene expression with antisense oligonucleotides or RNA interference (RNAi) mediated gene silencing by small interfering RNA (siRNA) has tremendous potential to silence the expression of disease-causing genes in the clinic.Author: Saeed Akhtar
https://www.sciencedirect.com/science/article/abs/pii/S0168365912005378
The promise of short RNA or DNA segments such as siRNAs, antisense oligonucleotides, and transcription factor decoys to treat disease has prompted nearly 40 clinical trials for RNA interference (RNAi)-based therapeutics and more than 100 clinical trials for antisense oligonucleotide-based technologies; in fact, there are promising in vivo and preclinical studies for many hundreds of technologies. Current treatment strategies are largely injection-based, so effective oral delivery …Author: Diane C. Forbes, Nicholas A. Peppas
https://www.sciencedirect.com/science/article/pii/S0168365912005378
Small interfering RNA (siRNA), microRNA (miRNA), antisense oligonucleotides (AS-ODNs), and transcription factor decoys are oligonucleotides that can regulate gene expression when delivered to the cytosol . These four strategies all use a short sequence of nucleotides (approximately 20 base pairs), and each strategy requires intracellular delivery and endosomal escape of the oligonucleotides.Author: Diane C. Forbes, Nicholas A. Peppas
https://www.sciencedirect.com/science/article/pii/S0022354916324522
Oral absorption of the 2′‐O‐(2‐methoxyethyl) modified antisense oligonucleotide (2′‐MOE ASO), ISIS 104838, was demonstrated in healthy volunteers with an average 9.5% plasma bioavailability across four formulations tested. The greatest average performance achieved in this study for a single formulation was 12.0% bioavailability within an individual dose and subject range of 1.96–27.5%.Author: Lloyd G. Tillman, Richard S. Geary, Gregory E. Hardee
https://www.cell.com/molecular-therapy-family/nucleic-acids/pdf/S2162-2531(16)30083-X.pdf
Delivery of Antisense Oligonucleotides Järver et al 2 initiation or elongation and thus decrease the levels of the cor-responding protein (Figure 1a). Steric blocking of ribosomal elongation is known to be hard to achieve, but blocking of ribo-somal initiation can be efficient by targeting the initiator AUG
https://www.sciencedirect.com/science/article/pii/S0168365908006834
Mar 04, 2009 · siRNA and antisense oligonucleotides, AON, have similar size and negative charge and are often packaged for in vitro delivery with cationic lipids or polymers—but exposed positive charge is problematic in vivo. Here we demonstrate loading and functional delivery of RNAi and AON with non-ionic, nano-transforming polymersomes.Author: Younghoon Kim, Manorama Tewari, J. David Pajerowski, Shenshen Cai, Shamik Sen, Jason Williams, Shash...
https://www.researchgate.net/publication/6118301_Oral_delivery_of_antisense_oligonucleotides_in_man
Oral drug delivery is the most patient-friendly route of administration but developing an effective delivery system for oligonucleotides remains a major challenge.
https://www.academia.edu/7664024/Polymersome_delivery_of_siRNA_and_antisense_oligonucleotides
Polymersome delivery of siRNA and antisense oligonucleotides
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