期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 10, 期 25, 页码 4954-4960出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c2ob25490e
关键词
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资金
- Science Foundation Ireland [07/SRC/B1154]
- Irish Drug Delivery Network
- Irish Research Council for Science, Engineering and Technology
- Science Foundation Ireland (SFI) [07/SRC/B1154] Funding Source: Science Foundation Ireland (SFI)
A new approach to the synthesis of amphiphilic beta-cyclodextrins has used 'click' chemistry to selectively modify the secondary 2-hydroxyl group. The resulting extended polar groups can be either polycationic or neutral PEGylated groups and these two amphiphile classes are compatible in dual cyclodextrin formulations for delivery of siRNA. When used alone with an siRNA, a cationic cyclodextrin was shown to have good transfection properties in cell culture. Co-formulation with a PEGylated cyclodextrin altered the physicochemical properties of nanoparticles formed with siRNA. Improved particle properties included lower surface charges and reduced tendency to aggregate. However, as expected, the transfection efficiency of the cationic vector was lowered by co-formulation with the PEGylated cyclodextrin, requiring future surface modification of particles with targeting ligands for effective siRNA delivery.
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