Abstract

Recently, various cyclodextrin (CyD)-grafted polymers and supramolecules have been developed as gene and oligonucleotide carriers. We have demonstrated that among the various polyamidoamine starburst^TM dendrimers (dendrimers) conjugates with CyDs (CDEs), the dendrimer (G2 or G3) conjugate with α-CyD showed high gene and oligonucleotide transfer activity with negligible cytotoxicity. In addition, to develop tissue- or cell-specific gene transfer carriers, we also prepared α-CDEs modified with functional molecules, such as mannose, fucose, galactose, lactose, polyethylene glycol (PEG) and folate-PEG. Moreover, polypseudorotaxane-appended α-CDEs were developed as sustained release systems for DNA and siRNA. Interestingly, glucronylglucosyl-β-CyD conjugates with dendrimer (G2) (GUG-β-CDE (G2)) showed high gene transfer activity compared to α-CDE (G2) and β-CDE (G2). In this review, we focus on the potential use of various CDEs as DNA and oligonucleotide transfer carriers.

Keywords: Cyclodextrin, polyamidoamine dendrimer, gene, oligonucleotide, sugars, folic acid, polypseudorotaxane.