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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.sigmaaldrich.com/catalog/papers/17721945
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...
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.deepdyve.com/lp/wiley/oral-delivery-of-antisense-oligonucleotides-in-man-ETNbgGmULL
Jan 01, 2008 · Oral delivery of antisense oligonucleotides in man This report describes, for the first time, the effective oral delivery of a second generation oligonucleotide where significant milligram amounts of intact drug are absorbed in human subjects.
https://www.future-science.com/doi/pdfplus/10.4155/tde.11.143
drug accumulation after oral feeding of an LNA antisense oligonucleotide directed against apoB-100. Presented at: Arteriosclerosis, Thrombosis and Vascular Biology. San Francisco, CA, USA, April 2010. 2 Aouadi M, Tesz GJ, Nicoloro SM et al. Orally delivered siRNA targeting macrophage Map4k4 suppresses systemic inflammation.
https://www.ncbi.nlm.nih.gov/pubmed/19530907
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
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