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Issue 47, 2016
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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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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.

Graphical abstract: 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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Article information


Submitted
15 Aug 2016
Accepted
21 Oct 2016
First published
15 Nov 2016

This article is Open Access

Polym. Chem., 2016,7, 7204-7210
Article type
Communication

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

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