Delivery of antisense oligonucleotides using cholesterol-modified sense dendrimers and cationic lipids.
Cholesterol modified mono-, di-, and tetrameric oligonucleotides were synthesized and hybridized with antisense oligonucleotides to study their incorporation in cationic liposomes together with the influence of this dendrimeric delivery system on biological activity. Electrostatic interactions seem to play the most important role during complexation with cationic lipids. This oligonucleotide formulation gives a small but significant increase in the inhibition of P-glycoprotein expression in a cellular system.
Chaltin
Patrick
P
Laboratory for Medicinal Chemistry, Rega Institute, Catholic University of Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium.
Margineanu
Anca
A
Marchand
Damien
D
Van Aerschot
Arthur
A
Rozenski
Jef
J
De Schryver
Frans
F
Herrmann
Andreas
A
Müllen
Klaus
K
Juliano
Rudolph
R
Fisher
Michael H
MH
Kang
Hyunmin
H
De Feyter
Steven
S
Herdewijn
Piet
P
D016475:3T3 Cells; D000818:Animals; D002412:Cations; D002784:Cholesterol / Q000737:chemistry*; D031541:Fluorescence Resonance Energy Transfer; D008055:Lipids / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D051379:Mice; D016376:Oligonucleotides, Antisense / Q000008:administration & dosage* / Q000737:chemistry
D002412:Cations; D008055:Lipids; D016376:Oligonucleotides, Antisense; D002784:Cholesterol