title: Synthesis and characterization of cationic glycidyl-based poly(aminoester)-folic acid targeting conjugates and study on gene delivery.
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.
authors: Department of Occupational Safety and Hygiene, Chia-Nan University of Pharmacy and Science, 60 Erh-Jen Rd., Sec. 1, Jen-Te, Taiwan. paifeng@mail.chna.edu.tw
authors: Pai Feng
authors: PF
authors: Tsai
authors: Wei Yang
authors: WY
authors: Chang
authors: Yu Che
authors: YC
authors: Hsiao
authors: Kuo Jung
authors: KJ
authors: Li
authors: Min Da
authors: MD
authors: Shau
mesh_terms: D000818:Animals; D019556:COS Cells; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D004247:DNA / Q000737:chemistry / Q000235:genetics; D004587:Electrophoresis, Agar Gel; D005492:Folic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000633:toxicity; D049452:Green Fluorescent Proteins / Q000096:biosynthesis / Q000235:genetics; D006367:HeLa Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007202:Indicators and Reagents / Q000138:chemical synthesis* / Q000633:toxicity; D010316:Particle Size; D010957:Plasmids / Q000737:chemistry / Q000235:genetics; D011073:Polyamines / Q000138:chemical synthesis* / Q000633:toxicity; D011994:Recombinant Proteins / Q000096:biosynthesis / Q000235:genetics; D017186:Titrimetry; D014162:Transfection
chemical_list: D007202:Indicators and Reagents; D011073:Polyamines; D011994:Recombinant Proteins; D049452:Green Fluorescent Proteins; D004247:DNA; D005492:Folic Acid