Lu Xueguang, Zhang Ke
Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02115, USA.
Nano Res. 2018 Oct;11(10):5519-5534. doi: 10.1007/s12274-018-2131-8. Epub 2018 Jul 6.
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.
聚乙二醇化，即连接聚乙二醇（PEG），已被用于改善寡核苷酸疗法的药代动力学特性近30年。此前的努力主要集中在研究具有不同分子量、末端官能团以及可能的寡核苷酸功能化位点的线性或轻度支化PEG。最近对高度支化PEG（包括刷状、星状和胶束结构）的研究表明，其在细胞摄取、基因调控效率、副作用减少和生物分布等几个方面具有优异特性。本综述着重比较PEG结构对聚乙二醇化寡核苷酸的物理化学和生物学特性的影响。
