Cyclodextrin-based facial amphiphiles: assessing the impact of the hydrophilic–lipophilic balance in the self-assembly, DNA complexation and gene delivery capabilities

摘要: Exhaustive structure–efficacy relationship studies on nonviral gene delivery systems are often hampered by the ill-defined or polydisperse nature of formulations. Facial amphiphiles based rigid cage-type molecular scaffolds offer unique possibilities towards these studies. Taking advantage regioselective functionalization schemes, we have synthesized a library cationic cyclodextrin (CD) derivatives combining range hydrophilic and lipophilic domains. We scrutinized how hydrophilic–lipophilic balance (HLB) around CD scaffold determines their self-assembly capabilities DNA binding release abilities corresponding CD:DNA nanocomplexes (CDplexes). These features been ultimately correlated with to deliver reporter luciferase-encoding pDNA into COS-7 cells. The ensemble results demonstrates that fine tuning HLB is critical induce compaction CD-based facial transfection-productive CDplexes.