Abstract

The purpose of this study is to evaluate in vitro gene transfer activity of polyamidoamine (PAMAM) starburst dendrimer (generation 3, G3) conjugate with α-cyclodextrin (α-CDE conjugate (G3)) bearing mannose (Man-α-CDE conjugate (G3)) with the degree of substitution of the mannose moiety 10 (DSM 10) as a novel non-viral vector in NIH3T3 and HepG2 cells. Man-α-CDE conjugate (G3) was found to have much higher gene transfer activity than dendrimer and α-CDE conjugate in NIH3T3 and HepG2 cells, which are independent of the expression of cell-surface mannose receptors. Gene transfer activity of Man-α-CDE conjugate (G3) was highly serum-resistant compared to that of dendrimer and α-CDE conjugate. No cytotoxicity after transfection of the complex of pDNA with Man-α-CDE conjugate (G3) was observed and the transfection activity was much higher than Lipofectin® in NIH3T3 cells. These results suggest the potential use of Man-α-CDE conjugate (G3) as a non-viral vector.

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