1. Impact of lipid substitution on assembly and delivery of siRNA by cationic polymers.
- Author
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Aliabadi HM, Landry B, Bahadur RK, Neamnark A, Suwantong O, and Uludağ H
- Subjects
- ATP Binding Cassette Transporter, Subfamily B, Member 1 genetics, ATP Binding Cassette Transporter, Subfamily B, Member 1 metabolism, Cell Line, Drug Carriers, Drug Stability, Glyceraldehyde-3-Phosphate Dehydrogenases genetics, Glyceraldehyde-3-Phosphate Dehydrogenases metabolism, Humans, Particle Size, Polyelectrolytes, Polyethyleneimine toxicity, RNA Interference, RNA, Small Interfering chemistry, Small Molecule Libraries, Lipids chemistry, Polyamines chemistry, Polyethyleneimine chemistry, RNA, Small Interfering administration & dosage, Transfection methods
- 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.)
- Published
- 2011
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