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Cyclodextrin/Dendrimer Conjugates as DNA and Oligonucleotide Carriers

[ Vol. 14 , Issue. 4 ]


Hidetoshi Arima, Keiichi Motoyama and Taishi Higashi   Pages 465 - 477 ( 13 )


Recently, various cyclodextrin (CyD)-grafted polymers and supramolecules have been developed as gene and oligonucleotide carriers. We have demonstrated that among the various polyamidoamine starburstTM 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.


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


Graduate School of Pharmaceutical Sciences, Kumamoto University, 5-1 Oe-honmachi, Chuo-ku, Kumamoto 862-0973, Japan

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