Pharmacokinetics and stability in the blood in vivo of phosphodiester and modified oligonucleotide derivatives
Laktionov, P.P.; Bryksin, A.V.; Rykova, E.I.; Amirkhanov, N.V.; Vlasov, V.V.
Voprosy Meditsinskoi Khimii 45(3): 206-215
1999
ISSN/ISBN: 0042-8809 PMID: 10432555 Document Number: 501688
In vivo stability and distribution of deoxyribooligonucleotides and 3'-end modified oligodeoxyribooligonucleotides were studied in blood serum and cells. Substitution of two 3'-end internucleotide phosphodiester bonds increased the stability of modified oligonucleotides. Modified oligonucleotides were shown to be stable in blood serum for up to 24 hours. Leukocytes did not bind oligonucleotides significantly, whereas erythrocytes accumulate mono-, di-, three-, tetranucleotides appeared in the blood stream as degradation products of the parent oligonucleotide.