PEGylation

This article is about PEGylation in a pharmaceutical context. For the bulk industrial process, see Ethoxylation.
Polyethylene glycol

PEGylation (or pegylation) is the process of both covalent and non-covalent attachment or amalgamation of polyethylene glycol (PEG, in pharmacy called macrogol) polymer chains to molecules and macrostructures, such as a drug, therapeutic protein or vesicle, which is then described as PEGylated.[1][2][3][4] PEGylation affects the resulting derivatives or aggregates interactions, which typically slows down their coalescence and degradation as well as elimination in vivo.[5][6]

PEGylation is routinely achieved by the incubation of a reactive derivative of PEG with the target molecule. The covalent attachment of PEG to a drug or therapeutic protein can "mask" the agent from the host's immune system (reducing immunogenicity and antigenicity), and increase its hydrodynamic size (size in solution), which prolongs its circulatory time by reducing renal clearance. PEGylation can also provide water solubility to hydrophobic drugs and proteins. Having proven its pharmacological advantages and acceptability, PEGylation technology is the foundation of a growing multibillion-dollar industry.[7]

  1. ^ Jokerst, Jesse V; Lobovkina, Tatsiana; Zare, Richard N; Gambhir, Sanjiv S (June 2011). "Nanoparticle PEGylation for imaging and therapy". Nanomedicine. 6 (4): 715–728. doi:10.2217/nnm.11.19. PMC 3217316. PMID 21718180.
  2. ^ Knop, Katrin; Hoogenboom, Richard; Fischer, Dagmar; Schubert, Ulrich S. (23 August 2010). "Poly(ethylene glycol) in Drug Delivery: Pros and Cons as Well as Potential Alternatives". Angewandte Chemie International Edition. 49 (36): 6288–6308. doi:10.1002/anie.200902672. PMID 20648499.
  3. ^ Veronese, Francesco M; Mero, Anna (2008). "The Impact of PEGylation on Biological Therapies". BioDrugs. 22 (5): 315–329. doi:10.2165/00063030-200822050-00004. PMID 18778113. S2CID 23901382.
  4. ^ Veronese, Francesco M.; Pasut, Gianfranco (November 2005). "PEGylation, successful approach to drug delivery". Drug Discovery Today. 10 (21): 1451–1458. doi:10.1016/S1359-6446(05)03575-0. PMID 16243265.
  5. ^ Blume G, Cevc, G (13 April 1990). "Liposomes for the sustained drug release in vivo". Biochimica et Biophysica Acta (BBA) - Biomembranes. 1029 (1): 91–97. doi:10.1016/0005-2736(90)90440-y. PMID 2223816.
  6. ^ Klibanov AL, Maruyama K, Torchilin VP, Huang L (30 July 1990). "Amphipathic polyethyleneglycols effectively prolong the circulation time of liposomes". FEBS Lett. 268 (1): 235–237. doi:10.1016/0014-5793(90)81016-h. PMID 2384160. S2CID 11437990.
  7. ^ Damodaran V. B.; Fee C. J. (2010). "Protein PEGylation: An overview of chemistry and process considerations". European Pharmaceutical Review. 15 (1): 18–26.{{cite journal}}: CS1 maint: multiple names: authors list (link)