"PEGylation of therapeutic oligonucletides: From linear to highly branc" by Xueguang Lu and Ke Zhang

Article Title

PEGylation of therapeutic oligonucletides: From linear to highly branched PEG architectures

Authors

Xueguang Lu, Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, USA
Ke Zhang, Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, USA

Keywords

PEGylation, oligonucleotide, brush polymer, antisense, small interfering RNA, aptamer, phosphorothioate

Abstract

ABSTRACT 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.