Lipidoligonucleotide conjugates as responsive nanomaterials for drug delivery

Abstract

We report Lipid OligoNucleotide conjugates (LONs) bearing either two or three hydrophobic chains. LONs self-assemble into micellar aggregates, which provide a suitable reservoir for hydrophobic drugs such as paclitaxel. Our results demonstrate that the composition of the LONs both in terms of the lipid and the oligonucleotide sequence impacts their ability to host lipophilic molecules. Interestingly, binding of the complementary oligonucleotide selectively induces the release of part of the drug payload of the aggregates. These LON based micelles, which efficiently host hydrophobic drugs, represent an original stimuli-responsive drug delivery system.