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

Felicity Heath; Amy Newman; Chiara Clementi; Gianfranco Pasut; Hong Lin; Gary J. Stephens; Benjamin J. Whalley; Helen M. I. Osborn; Francesca Greco

doi:10.1039/C6PY01418F

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

Felicity Heath,^a Amy Newman,^a Chiara Clementi,^b Gianfranco Pasut,^b Hong Lin,^a Gary J. Stephens,^a Benjamin J. Whalley,^a Helen M. I. Osborn^a and Francesca Greco*^a

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* Corresponding authors

^a Reading School of Pharmacy, PO Box 224, Reading, UK
E-mail: f.greco@reading.ac.uk

^b Dept. of Pharmaceutical Sciences, Via F. Marzolo 5, University of Padua, Padova, Italy

Abstract

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.

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Article information

DOI: https://doi.org/10.1039/C6PY01418F
Article type: Communication
Submitted: 15 Aug 2016
Accepted: 21 Oct 2016
First published: 15 Nov 2016
This article is Open Access

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Polym. Chem., 2016,7, 7204-7210

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

F. Heath, A. Newman, C. Clementi, G. Pasut, H. Lin, G. J. Stephens, B. J. Whalley, H. M. I. Osborn and F. Greco, Polym. Chem., 2016, 7, 7204 DOI: 10.1039/C6PY01418F

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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Polymer Chemistry

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

Abstract

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

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