A novel PEG–haloperidol conjugate with a non-degradable linker shows the feasibility of using polymer–drug conjugates in a non-prodrug fashion

Heath, F., Newman, A., Clementi, C., Pasut, G., Lin, H., Stephens, G. J. ORCID: https://orcid.org/0000-0002-8966-4238, Whalley, B. J., Osborn, H. M. I. ORCID: https://orcid.org/0000-0002-0683-0457 and Greco, F. (2016) A novel PEG–haloperidol conjugate with a non-degradable linker shows the feasibility of using polymer–drug conjugates in a non-prodrug fashion. Polymer Chemistry, 7 (47). pp. 7204-7210. ISSN 1759-9954 doi: 10.1039/c6py01418f

Abstract/Summary

A PEG–haloperidol conjugate containing a non-biodegradable linker was synthesised. Incubation with rat plasma demonstrated excellent linker stability, and competition radioligand binding assays demonstrated retained binding to the D2-receptor. In silico studies predicted that the conjugate will not cross the blood–brain barrier (BBB), thus potentially restricting haloperidol action to one side of the BBB.

Item Type	Article
URI	https://reading-clone.eprints-hosting.org/id/eprint/68375
Identification Number/DOI	10.1039/c6py01418f
Refereed	Yes
Divisions	Interdisciplinary centres and themes > Chemical Analysis Facility (CAF) Life Sciences > School of Chemistry, Food and Pharmacy > School of Pharmacy > Medicinal Chemistry Research Group Life Sciences > School of Chemistry, Food and Pharmacy > School of Pharmacy > Division of Pharmacology Life Sciences > School of Chemistry, Food and Pharmacy > School of Pharmacy > Pharmaceutics Research Group
Publisher	Royal Society of Chemistry
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