Folic acid (FA) has high affinity to folate receptors (FRs), which have three
isoforms: FRα, FRβ and FRγ. Among them, FRα is a tumor specific receptor, as it is
frequently over-expressed in diverse malignancies but not in normal tissues. In this
study, we have conjugated FA to a chitosan-poly(ethylenimine) copolymer, and have
confirmed the low cytotoxicity of the product (namely “CP1.3K-FA”) in cancer cells.
The transfection efficiency of CP1.3K-FA has been shown by the EGFP transfection
assay to be higher than that of the unmodified chitosan-poly(ethylenimine) copolymer under optimal conditions. Results
of the luciferase activity assay have also indicated that the transfection efficiency of CP1.3K-FA is comparable to that of
Fugene HD in B16 and U87 cells. Our results have suggested that CP1.3K-FA warrants further development as a vector
for gene delivery in cancer cells.
Keywords: Chitosan, Folic acid, Gene transfer, Non-viral vectors, Poly(ethylenimine), Targeting.
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