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Molecules 2012, 17(8), 9056-9069; doi:10.3390/molecules17089056

Synthesis and Characterization of Cationic Glycidyl-Based Poly(aminoester)-Folic Acid Targeting Conjugates and Study on Gene Delivery

Received: 24 May 2012 / Revised: 18 July 2012 / Accepted: 21 July 2012 / Published: 30 July 2012
(This article belongs to the Section Medicinal Chemistry)
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A new poly(aminoester) (EPAE-FA) containing folic acid and amino groups in the backbone and side chain was synthesized. EPAE-FA self-assembled readily with the plasmid DNA (pCMV-βgal) in HEPES buffer and was characterized by dynamic light scattering, zeta potential, fluorescence images, and XTT cell viability assays. To evaluate the transfection effect of graft ratio of FA on the EPAE system, EPAE-FA polymers with two different graft ratios (EPAE-FA12k and EPAE-FA14k) were also prepared. This study found that all EPAE-FA polymers were able to bind plasmid DNA and yielded positively charged complexes with nano-sized particles ( < 200 nm). To assess the transfection efficiency mediated by EPAE and EPAE-FA polymers, we performed in vitro transfection activity assays using FR-negative (COS-7) and FR-positive (HeLa) cells. The EPAE-FA12k/DNA and EPAE-FA14k/DNA complexes were able to transfect HeLa cell in vitro with higher transfection efficiency than PEI25k/DNA at the similar weight ratio. These results demonstrated that the introduction of FA into EPAE system had a significant effect on transferring ability for FR-positive cells (HeLa). Examination of the cytotoxicity of PEI25k and EPAE-FA system revealed that EPAE-FA system had lower cytotoxicity. In this paper, EPAE-FA seemed to be a novel cationic poly(aminoester) for gene delivery and an interesting candidate for further study.
Keywords: poly(aminoester); folic acid; transfection; cytotoxicity poly(aminoester); folic acid; transfection; cytotoxicity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Tsai, P.F.; Chang, W.Y.; Hsiao, Y.C.; Li, K.J.; Shau, M.D. Synthesis and Characterization of Cationic Glycidyl-Based Poly(aminoester)-Folic Acid Targeting Conjugates and Study on Gene Delivery. Molecules 2012, 17, 9056-9069.

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