Tools for PEGylation

Matthias Junkers

Polyethylene glycol (PEG) reagents offer numerous favorable characteristics, including high water solubility, high mobility in solution, lack of toxicity and immunogenicity, and ready clearance from the body. Thus, the chemical modification of biologically active compounds, such as peptides, antibody fragments, enzymes, or small molecules with polyethylene glycol chains (referred to as PEGylation), is an effective method to tailor molecular properties to particular applications (Figure 1).

Figure 1. Tools for PEGylation

Drugs can especially benefit from PEGylation as has been proved by a continuously growing number of PEG conjugated drugs on the market. By increasing the molecular mass of proteins and peptides and shielding them from proteolytic enzymes, PEGylation improves pharmacokinetics.¹ The judicious choice of PEG size and linkers enhance a potential drug’s solubility and its distribution within an organism.²

Numerous review articles concerning the application of PEG polymers in drug delivery are available.^3-6 In some recent reports PEGylation is discussed as a tool to facilitate the drug delivery of nanocarrier systems and microparticles.^7,8

We are proud to further expand our offering of tools for PEGylation with new bifunctional, small and medium-sized poly(ethylene glycol) building blocks. Please visit our online product catalog for a complete list of PEGylation products.

References

1. Harris JM, Chess RB. 2003. Effect of pegylation on pharmaceuticals. Nat Rev Drug Discov. 2(3):214-221. https://doi.org/10.1038/nrd1033

2. Fee CJ. 2007. Size comparison between proteins PEGylated with branched and linear poly(ethylene glycol) molecules. Biotechnol. Bioeng.. 98(4):725-731. https://doi.org/10.1002/bit.21482

3. Veronese FM. 2001. Peptide and protein PEGylation. Biomaterials. 22(5):405-417. https://doi.org/10.1016/s0142-9612(00)00193-9

4. Roberts M, Bentley M, Harris J. 2002. Chemistry for peptide and protein PEGylation. Advanced Drug Delivery Reviews. 54(4):459-476. https://doi.org/10.1016/s0169-409x(02)00022-4

5. Veronese FM, Pasut G. 2005. PEGylation, successful approach to drug delivery. Drug Discovery Today. 10(21):1451-1458. https://doi.org/10.1016/s1359-6446(05)03575-0

6. Ryan SM, Mantovani G, Wang X, Haddleton DM, Brayden DJ. 2008. Advances in PEGylation of important biotech molecules: delivery aspects. Expert Opinion on Drug Delivery. 5(4):371-383. https://doi.org/10.1517/17425247.5.4.371

7. Howard MD, Jay M, Dziubla TD, Lu X. 2008. PEGylation of Nanocarrier Drug Delivery Systems: State of the Art. Journal of Biomedical Nanotechnology. 4(2):133-148. https://doi.org/10.1166/jbn.2008.021

8. Wattendorf U, Merkle HP. 2008. PEGylation as a tool for the biomedical engineering of surface modified microparticles. Journal of Pharmaceutical Sciences. 97(11):4655-4669. https://doi.org/10.1002/jps.21350