Poly(ethylene glycol) in Drug Delivery: Pros and Cons as Well as Potential Alternatives

Knop, Katrin; Hoogenboom, Richard; Fischer, Dagmar; Schubert, Ulrich S.

doi:10.1002/anie.200902672

Cited by 3,533Nanoparticle-Based Drug DeliveryAdvanced Drug Delivery SystemsDendrimers and Hyperbranched Polymers

Poly(ethylene glycol) in Drug Delivery: Pros and Cons as Well as Potential Alternatives

Knop, Katrin, Hoogenboom, Richard, Fischer, Dagmar, Schubert, Ulrich S.·2010·Angewandte Chemie International Edition

DOI 10.1002/anie.200902672

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Abstract

Poly(ethylene glycol) (PEG) is the most used polymer and also the gold standard for stealth polymers in the emerging field of polymer‐based drug delivery. The properties that account for the overwhelming use of PEG in biomedical applications are outlined in this Review. The first approved PEGylated products have already been on the market for 20 years. A vast amount of clinical experience has since been gained with this polymer—not only benefits, but possible side effects and complications have also been found. The areas that might need consideration and more intensive and careful examination can be divided into the following categories: hypersensitivity, unexpected changes in pharmacokinetic behavior, toxic side products, and an antagonism arising from the easy degradation of the polymer under mechanical stress as a result of its ether structure and its non‐biodegradability, as well as the resulting possible accumulation in the body. These possible side effects will be discussed in this Review and alternative polymers will be evaluated.

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PEG immunogenicity depends on the degree of PEGylation to which the molecule it is coupled with, and PEG has been shown to induce unpredictable complement activation.
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From Lipid nanoparticles for mRNA delivery (2021) · cites this paper as [127]
Numerous natural and synthetic polymers have been investigated as alternatives to PEG, several of which are under evaluation in clinical trials.
“To ameliorate safety concerns, numerous natural and synthetic polymers have been investigated as alternatives to PEG, of which several are under evaluation in clinical trials127,169.”
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Authors: Knop, K., Hoogenboom, R., Fischer, D., & Schubert, U. S.
Affiliations: Dutch Polymer Institute (NL)
Friedrich Schiller University Jena (DE)
ORCID: Hoogenboom, Richard
Fischer, Dagmar
Schubert, Ulrich S.
Venue: Angewandte Chemie International Edition
Publisher: Wiley
Published: 2010-07-20
Volume: 49
Issue: 36
Pages: 6288-6308
ISSN: 1433-7851 (ISSN-L)
1521-3773
DOI: 10.1002/anie.200902672
OpenAlex: W2164841185
Cited by: 3,533
References: 219
Citations by year: 2026: 176 · 2025: 207 · 2024: 191 · 2023: 213 · 2022: 255 · 2021: 270 · 2020: 259 · 2019: 260 · 2018: 277 · 2017: 234 · 2016: 275 · 2015: 254 · 2014: 206 · 2013: 180 · 2012: 159
FWCI: 7.02
Type: journal article
Language: en
Open access: closed
Licence: onlinelibrary.wiley.com/termsAndConditions#vor (vor)
Locations: Angewandte Chemie International Edition (publishedVersion)
PubMed (publishedVersion)
Ghent University Academic Bibliography (Ghent University) (submittedVersion)
DIAL (Catholic University of Leuven) (submittedVersion)
Topics: Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
Physical Sciences › Materials Science › Polymers and Plastics › Dendrimers and Hyperbranched Polymers
Keywords: polyethylene glycol, PEGylation, stealth polymers, polymeric drug delivery, hypersensitivity, pharmacokinetics, polymer degradation
MeSH terms: Biocompatible Materials, Drug Carriers, Pharmaceutical Preparations, Polyethylene Glycols, Polymers

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Poly(ethylene glycol) in Drug Delivery: Pros and Cons as Well as Potential Alternatives

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