Abstract
Characterization of a polymer library engineered to enhance their ability to protect and deliver their nucleotide cargo to the cells is reported. The ζ-potential continuously increased with higher polymer:siRNA weight ratio, and the ζ-potential of lipid-modified polymers:siRNA complexes were higher than PEI2 at all ratios. At polymer:siRNA ratio of 1:1, all lipid-substituted polymers showed complete protection against degradation. Lipid-modified polymers significantly increased the cellular uptake of siRNA complexes and down-regulation of GAPDH and P-gp (max. 66% and 67%, respectively). The results indicate that hydrophobic modification of low molecular PEI could render this otherwise ineffective polymer to a safe effective delivery system for intracellular siRNA delivery and protein silencing.
Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
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Cell Line
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Drug Carriers
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Drug Stability
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Glyceraldehyde-3-Phosphate Dehydrogenases / genetics
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Glyceraldehyde-3-Phosphate Dehydrogenases / metabolism
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Humans
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Lipids / chemistry*
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Particle Size
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Polyamines / chemistry*
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Polyelectrolytes
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Polyethyleneimine / chemistry*
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Polyethyleneimine / toxicity
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RNA Interference
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RNA, Small Interfering / administration & dosage*
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RNA, Small Interfering / chemistry
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Small Molecule Libraries
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Transfection / methods*
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Drug Carriers
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Lipids
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Polyamines
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Polyelectrolytes
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RNA, Small Interfering
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Small Molecule Libraries
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polycations
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Polyethyleneimine
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Glyceraldehyde-3-Phosphate Dehydrogenases