Simberg Dmitri, Barenholz Yechezkel, Roffler Steve R, Landfester Katharina, Kabanov Alexander V, Moghimi Seyed M
Department of Pharmaceutical Sciences, The Skaggs School of Pharmacy and Pharmaceutical Sciences and Colorado Center for Nanomedicine and Nanosafety, University of Colorado Anschutz Medical Campus, Aurora, CO, USA.
Translational Bio-Nanosciences Laboratory, Department of Pharmaceutical Sciences, Skaggs School of Pharmacy, University of Colorado Anschutz Medical Campus, Aurora, CO, USA.
Drug Deliv. 2025 Dec;32(1):2494775. doi: 10.1080/10717544.2025.2494775. Epub 2025 Apr 23.
PEGylation technology, that is grafting of poly(ethylene glycol)(PEG) to biologics, vaccines and nanopharmaceuticals, has become a cornerstone of modern medicines with over thirty products used in the clinic. PEGylation of therapeutic proteins, nucleic acids and nanopharmaceuticals improves their stability, pharmacokinetic and biodistribution. While PEGylated medicines are safe in the majority of patients, there are growing concerns about the emergence of anti-PEG antibodies and their impact on the therapeutic efficacy of PEGylated medicines as well as broader immune responses, particularly in complement activation and hypersensitivity reactions. These concerns are beginning to scrutinize the future viability of PEGylation technology in medicine design. Here, we outline these concerns, encourage more efforts into looking for comprehensive scientific evidence on the role of anti-PEG antibodies in hypersensitivity reactions, discuss alternatives to PEG and propose strategies for moving PEGylation technology forward.
聚乙二醇化技术,即将聚乙二醇(PEG)接枝到生物制品、疫苗和纳米药物上,已成为现代医学的基石,有三十多种产品应用于临床。治疗性蛋白质、核酸和纳米药物的聚乙二醇化可提高它们的稳定性、药代动力学和生物分布。虽然聚乙二醇化药物在大多数患者中是安全的,但人们越来越担心抗PEG抗体的出现及其对聚乙二醇化药物治疗效果的影响,以及更广泛的免疫反应,特别是在补体激活和超敏反应方面。这些担忧开始审视聚乙二醇化技术在药物设计中的未来可行性。在此,我们概述这些担忧,鼓励更多努力去寻找关于抗PEG抗体在超敏反应中作用的全面科学证据,讨论PEG的替代物,并提出推动聚乙二醇化技术向前发展的策略。