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

Molecules

Pai Feng Tsai³  Wei Yang Chang²  Yu Che Hsiao¹  Kuo Jung Li² 

[1] Department of Materials Science and Engineering, University of Tennessee, Knoxville, TN 37996, USA;Department of Biotechnology, Chia-Nan University of Pharmacy and Science, 60 Erh-Jen Rd., Sec. 1, Jen-Te, Taiwan;Department of Occupational Safety and Hygiene, Chia-Nan University of Pharmacy and Science, 60 Erh-Jen Rd., Sec. 1, Jen-Te, Taiwan;

关键词: poly(aminoester);    folic acid;    transfection;    cytotoxicity;   

DOI  :  10.3390/molecules17089056

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2012 by the authors; licensee MDPI, Basel, Switzerland.