聚乙二醇化
乙二醇
PEG比率
分散性
组合化学
化学
聚乙二醇
小分子
聚合物
药品
高分子
共价键
脂质体
纳米技术
核酸
材料科学
药理学
有机化学
生物化学
生物
经济
财务
作者
Jinming Hu,Shiyong Liu
标识
DOI:10.1016/j.cobme.2022.100419
摘要
PEGylation refers to a general approach in drug development by covalently or noncovalently attaching poly (ethylene glycol) (PEG) to small molecule drugs, contrast agents, proteins, nucleic acids, liposomes, etc. This strategy endows the resulting PEGylated drugs with increased water dispersity, stability, and optimized pharmacokinetics and pharmacodynamics. However, conventional narrowly dispersed PEG is indeed a polymer mixture, which can complicate the synthesis and purification of PEGylated drugs and elicit unwanted immunogenic reactions, eventually compromising therapeutic outcomes. To circumvent these drawbacks, discrete PEG (dPEG) with identical chemical structures but precise molecular weights to conventional polydisperse PEG has been developed, enabling the construction of dPEGylated drugs. Preliminary results suggest that dPEGylated drugs can efficiently overcome the molecular heterogeneity and immunogenic issue of conventional PEGylated drugs, representing a new direction in the development of precision macromolecular drugs.
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