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Cross-linked polymers with fluorinated bridge for efficient gene delivery


A new strategy for the construction of fluorinated cationic polymers for gene delivery was introduced. The fluorinated polymers were synthesized by crosslinking low molecular weight PEI with diols containing various lengths of perfluoroalkyl chain via epoxide ring-opening polymerization. Such study presents the first example for the polymeric gene vectors with fluorination on the polymer backbone but not side chain. These materials showed good DNA condensation and protection ability and could condense DNA into nanoparticles with proper sizes and zeta-potentials. The fluorine atoms might strengthen the interaction toward DNA, leading to more stable polyplexes. In vitro transfection results showed that the fluorinated polymers could mediate efficient gene delivery toward both 2D and 3D cell culture at low weight ratio, and the transfection efficiency was higher than PEI 25 kDa and the non-fluorinated counterpart. Several assays including DLS, TEM, luciferase reporter gene transfection and flow cytometry revealed that fluorination improved the serum resistance of these polymeric vectors, and more fluorine atoms might lead to better serum tolerance. These fluorinated materials exhibited very low cytotoxicity at transfection dosage. Cellular uptake study with uptake inhibitors indicated that macro-pinocytosis and microtubule-mediated endocytosis were the major endocytosis pathways for these polyplexes.

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Publication details

The article was received on 12 Aug 2017, accepted on 09 Oct 2017 and first published on 09 Oct 2017

Article type: Paper
DOI: 10.1039/C7TB02158E
Citation: J. Mater. Chem. B, 2017, Accepted Manuscript
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    Cross-linked polymers with fluorinated bridge for efficient gene delivery

    X. Yu, Y. Xiao, J. Zhang, Y. Liu, Z. Huang, B. Wang and Y. Zhang, J. Mater. Chem. B, 2017, Accepted Manuscript , DOI: 10.1039/C7TB02158E

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