作者:Oleksandr Pokholenko、Arnaud Gissot、Brune Vialet、Katell Bathany、Alain Thiéry、Philippe Barthélémy
DOI:10.1039/c3tb20357c
日期:——
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.
我们报告了带有两条或三条疏水链的脂质寡核苷酸共轭物(LONs)。LONs 可自组装成胶束聚集体,为紫杉醇等疏水性药物提供合适的储存库。我们的研究结果表明,LONs 在脂质和寡核苷酸序列方面的组成会影响其容纳亲脂分子的能力。有趣的是,互补寡核苷酸的结合会选择性地诱导聚集体中部分药物载荷的释放。这些基于 LON 的胶束能有效地容纳疏水性药物,是一种独创的刺激响应式给药系统。