Water-soluble block polycations as carriers for oligonucleotide delivery.

Important note: Information in this article was accurate in 1996. The state of the art may have changed since the publication date.

Water-soluble block polycations as carriers for oligonucleotide delivery.

Bioconjug Chem. 1995 Nov-Dec;6(6):639-43. Unique Identifier : AIDSLINE MED/96167451
Kabanov AV; Vinogradov SV; Suzdaltseva YG; Alakhov VYu; Moscow Institute of Biotechnology, Inc., Faculty of Chemistry,; Moscow State University, Vorobievy Gory, Russia.

Abstract: Water-soluble, block copolymeric carriers consisting of polyoxyethylene (PEO) and polyspermine (PS) chains have been developed for the delivery of antisense oligonucleotides (oligo) into the target cells. These copolymers spontaneously form complexes with oligos in aqueous solutions. The PS block electrostatically binds to the oligo, and as a result, the stability of the oligo is increased. Similarly, the polar PEO block provides for the aqueous solubility of the complex. This paper (i) reports the synthesis of the diblock PEO-PS copolymer and (ii) evaluates the effects of the complexes formed between this copolymer and phosphodiester oligo, complementary to the splice junction of herpes simplex virus type 1 immediate early pre-mRNAs 4 and 5, on the reproduction of this virus in Vero cells. Infectious titer data 22 and 39 h post infection indicates that the copolymer-oligo complex inhibits the reproduction of the virus beyond the detection limit. Conversely, the free oligo inhibits the reproduction of the virus only 22 h postinfection, while 39 h postinfection significant virus titers are observed. The results of this study suggest that the copolymer complex increases the sequence-specific inhibition effect of oligo on the virus reproduction.

Keywords: Animal Antiviral Agents/ADMINISTRATION & DOSAGE/PHARMACOLOGY Base Sequence Cations Cercopithecus aethiops *Drug Carriers Drug Stability Electrochemistry Ethylenes/*CHEMISTRY HIV-1/DRUG EFFECTS/PHYSIOLOGY Molecular Sequence Data Oligonucleotides, Antisense/*ADMINISTRATION & DOSAGE/CHEMISTRY/ PHARMACOLOGY Polymers/*CHEMISTRY Solubility Spermine/*CHEMISTRY Vero Cells Virus Replication/DRUG EFFECTS Water JOURNAL ARTICLE
960830
M9681225

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