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Bioconjug Chem ; 17(3): 781-6, 2006.
Article in English | MEDLINE | ID: mdl-16704218

ABSTRACT

Diblock copolymers that consist of poly(2-ethyl-2-oxazoline) (PEOz) and linear polyethylenimine (LPEI) were prepared for use as nonviral gene carriers. The PEOz-b-LPEI copolymers were synthesized by coupling PEOz with LPEI in a thiol-disulfide exchange reaction between the sulfhydryl and pyridyl disulfide terminal groups. A polymer/DNA weight ratio (P/D) of over 12 was required to enable PEOz-b-LPEI to condense DNA completely. The DNA-condensing capability of the diblock copolymers was increased with increasing the hydrolytic degrees of the LPEI segment. The PEOz-b-LPEI polyplexes were stable in 150 mM NaCl aqueous solution and had a mean diameter around 190 nm, whereas BPEI and LPEI polyplexes formed large aggregates in the range 300-500 nm. In addition, these polyplexes exhibited the sensitivity to solution pH and were dissociated in the acidic buffers (pH < or = 5.5). The results of in vitro cell viability and luciferase assay indicated that PEOz-b-LPEI showed not only low cytotoxicity but also high transfection efficiency in gene expression.


Subject(s)
Oxazoles/chemistry , Polyethyleneimine/chemistry , Polymers/chemistry , Cell Survival/drug effects , DNA, Viral/genetics , Gene Expression , Genes, Reporter/genetics , Genetic Vectors/genetics , HeLa Cells , Humans , Hydrogen-Ion Concentration , Magnetic Resonance Spectroscopy , Molecular Structure , Oxazoles/chemical synthesis , Particle Size , Polyamines , Polyethyleneimine/toxicity , Polymers/chemical synthesis , Transfection
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