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

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

1 Department of Occupational Safety and Hygiene, Chia-Nan University of Pharmacy and Science, 60 Erh-Jen Rd., Sec. 1, Jen-Te, Taiwan 2 Department of Biotechnology, Chia-Nan University of Pharmacy and Science, 60 Erh-Jen Rd., Sec. 1, Jen-Te, Taiwan 3 Department of Materials Science and Engineering, University of Tennessee, Knoxville, TN 37996, USA
* Author to whom correspondence should be addressed.
Received: 24 May 2012; in revised form: 18 July 2012 / Accepted: 21 July 2012 / Published: 30 July 2012
(This article belongs to the Section Medicinal Chemistry)
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Abstract: 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

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MDPI and ACS Style

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.

AMA Style

Tsai PF, Chang WY, Hsiao YC, Li KJ, Shau MD. Synthesis and Characterization of Cationic Glycidyl-Based Poly(aminoester)-Folic Acid Targeting Conjugates and Study on Gene Delivery. Molecules. 2012; 17(8):9056-9069.

Chicago/Turabian Style

Tsai, Pai Feng; Chang, Wei Yang; Hsiao, Yu Che; Li, Kuo Jung; Shau, Min Da. 2012. "Synthesis and Characterization of Cationic Glycidyl-Based Poly(aminoester)-Folic Acid Targeting Conjugates and Study on Gene Delivery." Molecules 17, no. 8: 9056-9069.

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