Biological Engineering Institute of Zhejiang Chinese Medical University.
Biol Pharm Bull. 2014;37(3):335-9. doi: 10.1248/bpb.b13-00661. Epub 2013 Dec 12.
PEGylation changes the physical and chemical properties of the biomedical molecule, such as its conformation, electrostatic binding, and hydrophobicity, and results in an improvement in the pharmacokinetic behavior of the drug, while it also causes some disadvantages of which cannot be neglected. The available data manifests that polyethylene glycol (PEG) itself shows potential risk, such as immunogenicity of the PEG and PEG-containing vacuoles in cells observed with PEGylated biologicals. Decreased activity and heterogeneity are also the negative aspects of PEGylation. The unfavorable impacts which are brought by the PEGylation are described here with examples of modified therapeutic proteins on the market and used in the clinical trials.
聚乙二醇（PEG）化改变了生物医学分子的物理和化学性质，如构象、静电结合和疏水性，从而改善了药物的药代动力学行为，但也带来了一些不可忽视的缺点。现有数据表明，聚乙二醇（PEG）本身存在潜在风险，如 PEG 化生物制剂中观察到的 PEG 免疫原性和细胞中的 PEG 包含空泡。PEG 化也会导致活性降低和异质性。本文通过市场上修饰的治疗性蛋白和临床试验中使用的例子描述了 PEG 化带来的不利影响。
