Abstract
In this research, the inclusion complex of cationic β-cyclodextrins (bcd) and adamantane (Ad) conjugated poly (vinyl alcohol), PVA, containing a poly (ethylene glycol) (PEG) polymer or Ad-PVA-PEG has been designed and synthesized as a siRNA carrier. Three different amino groups, i.e., putrescine, spermidine, and spermine substituted β-cyclodextrin (bcd1-3), were prepared. Their chemical structures were confirmed by 1H NMR and mass analysis. PVA was substituted by 4-hydroxy benzaldehyde connected to adamantane, which can fit in the β-cyclodextrin cavity. PEG was attached to the PVA chain. From the experiments, three cationic β-cyclodextrins can form the spherical nanoparticles with siRNA and Ad-PVA-PEG, as confirmed by 1H NMR and SEM analysis. The nanoparticles of Ad-PVA-PEG and bcd1-3 with various ratios have been studied, including the siRNA binding efficiency using gel electrophoresis. The nanoparticle size and zeta potential were investigated by using dynamic light scattering (DLS). It was found that the average size of the particles was less than 300 nm in range with the negative zeta potential buffer pH 7.4. In vitro evaluation showed that the siRNA nanoparticles knocked down GFP expression in A549 cells. The cytotoxicity test of siRNA nanoparticles show the same trend with Lipofectamine® 2000. Therefore, the self-assembly cationic bcd with Ad-PVA-PEG containing siRNA was a safe and efficient system for siRNA delivery.
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