Abstract
Cationic amphiphilic polyester dendrimers possessing varied numbers of choline and alkyl chains on the periphery were synthesized and characterized. A combination of divergent and convergent synthetic routes was used to efficiently prepare the dendrimers. All of the amphiphiles bound DNA as determined by an ethidium bromide displacement assay, and the dendrimer that contained two choline and four alkyl chains exhibited the smallest charge ratio. Only this amphiphilic dendrimer formed a well-defined structure alone or with DNA in solution, while the other dendrimer compositions gave aggregates. Specifically, small vesicular structures of several 100 nanometers in diameter were observed with DNA, and this dendrimerplex exhibited the greatest transfection efficiency of the group. The results of this study highlight the important role that charge, hydrophobicity, size, and compaction ability play in binding and formation of DNA-dendrimer complexes and the resulting transfection efficiency. Cationic amphiphilic polyester dendrimers possessing different numbers of choline heads groups and myristic acid alkyl chains were synthesized and evaluated for gene transfection.
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