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Fine-tuned PEGylation of chitosan to maintain optimal siRNA-nanoplex bioactivity

  • Polyethylene glycol (PEG) is a widely used modification for drug delivery systems. It reduces undesired interaction with biological components, aggregation of complexes and serves as a hydrophilic linker of ligands for targeted drug delivery. However, PEGylation can also lead to undesired changes in physicochemical characteristics of chitosan/siRNA nanoplexes and hamper gene silencing. To address this conflicting issue, PEG-chitosan copolymers were synthesized with stepwise increasing degrees of PEG substitution (1.5% to 8.0%). Subsequently formed PEG-chitosan/siRNA nanoplexes were characterized physicochemically and biologically. The results showed that small ratios of chitosan PEGylation did not affect nanoplex stability and density. However, higher PEGylation ratios reduced nanoplex size and charge, as well as cell uptake and final siRNA knockdown efficiency. Therefore, we recommend fine-tuning of PEGylation ratios to generate PEG-chitosan/siRNA delivery systems with maximum bioactivity. The degree of PEGylation for chitosan/siRNA nanoplexes should be kept low in order to maintain optimal nanoplex efficiency.

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Author of HS ReutlingenKrastev, Rumen
Erschienen in:Carbohydrate polymers
Place of publication:Amsterdam
Document Type:Journal article
Publication year:2016
Tag:PEGylated chitosan; chitosan; gene silencing; nanoplex functionality; siRNA-delivery
Page Number:10
First Page:25
Last Page:34
DDC classes:540 Chemie
Open access?:Nein
Licence (German):License Logo  In Copyright - Urheberrechtlich geschützt