Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 78, Issue -, Pages 118-125Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.03.050
Keywords
Gene delivery; Polyester; Michael reaction; Polyethylenimine 600; Non-viral vector; Cationic polymer
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Funding
- National Program on Key Basic Research Project of China (973 Program) [2012CB720603]
- National Natural Science Foundation of China [21232005, J1103315]
- Specialized Research Fund for the Doctoral Program of Higher Education [20120181130006]
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Routine clinical implementation of human gene therapy requires safe and efficient gene delivery methods. Linear biodegradable polyesters with carbon-carbon double bonds are prepared from unsaturated diacids and diols. Subsequent appending of low molecular weight PEI by Michael addition gives target cationic polymers efficiently. Agarose gel retardation and fluorescence quenching assays show that these materials have good DNA binding ability and can completely retard plasmid DNA at weight ratio of 0.8. The formed polyplexes have appropriate sizes around 275 nm and zeta-potential values about +20 -35 mV. The cytotoxicities of these polymers assayed by MTT are much lower than that of 25 kDa PEI. In vitro transfection toward 7402, HEK293 and U-2OS cells show that polymer P1 may give dramatically higher transfection efficiency (TE) than 25 kDa PEI, especially in U-2OS cells, suggesting that such polymer might be promising non-viral gene vectors. (C) 2014 Elsevier Masson SAS. All rights reserved.
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