Laboratory of Therapeutic Innovation, UMR7200 CNRS-Université de Strasbourg, Faculté de Pharmacie , Illkirch 67401, France.
ACS Appl Mater Interfaces. 2016 Nov 16;8(45):30665-30670. doi: 10.1021/acsami.6b09365. Epub 2016 Nov 3.
A novel generation of pH-responsive photopolymerized diacetylenic amphiphile (PDA) micelles with a diameter of 10 nm was designed and optimized for the intracellular delivery of siRNAs. Dialysis and photopolymerization of the micelles allowed a strong reduction of the cytotoxicity of the nanovector, while the hydrophilic histidine headgroup permitted enhancing the siRNA delivery potential by improving the endosomal escape via imidazole protonation. These PDA-micellar systems were fully characterized by DLS, TEM, and DOSY-NMR experiments. The resulting bioactive complexes of PDA-micelles with siRNA were shown to have an optimal size below 100 nm.
一种新型的 pH 响应光聚合二炔基两亲性（PDA）胶束，其直径为 10nm，被设计并优化用于 siRNA 的细胞内递送。胶束的透析和光聚合允许强烈降低纳米载体的细胞毒性，而亲水性组氨酸头基允许通过咪唑质子化增强内涵体逃逸来提高 siRNA 递送潜力。这些 PDA 胶束系统通过 DLS、TEM 和 DOSY-NMR 实验进行了充分的表征。结果表明，PDA 胶束与 siRNA 的生物活性复合物的最佳尺寸低于 100nm。
