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PEGylation, the attachment of poly(ethylene glycol) (PEG), has been adopted to improve the pharmacokinetic properties of oligonucleotide therapeutics for nearly 30 years. Prior efforts mainly focused on the investigation of linear or slightly branched PEG having different molecular weights, terminal functional groups, and possible oligonucleotide sites for functionalization. Recent studies on highly branched PEG (including brush, star, and micellar structures) indicate superior properties in several areas including cellular uptake, gene regulation efficacy, reduction of side effects, and biodistribution. This review focuses on comparing the effects of PEG architecture on the physiochemical and biological properties of the PEGylated oligonucleotide.

Publication history
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Acknowledgements

Publication history

Received: 19 April 2018
Revised: 08 June 2018
Accepted: 18 June 2018
Published: 06 July 2018
Issue date: October 2018

Copyright

© Tsinghua University Press and Springer-Verlag GmbH Germany, part of Springer Nature 2018

Acknowledgements

Acknowledgements

Financial support by the National Institute of General Medical Sciences Award Number 1R01GM121612-01, the National Science Foundation (CAREER Award Number 1453255), and the American Chemical Society Petroleum Research Fund (No. PRF 54905-DNI5), is acknowledged.

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