Published in
Royal Society of Chemistry, Polymer Chemistry, 47(7), p. 7204-7210, 2016
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
Journal article published in 2016 by
Felicity Heath,
Amy Newman,
Chiara Clementi,
Gianfranco Pasut 
,
Hong Lin,
Gary J. Stephens,
Benjamin J. Whalley,
Helen M. I. Osborn ,
Francesca Greco
,
Hong Lin,
Gary J. Stephens,
Benjamin J. Whalley,
Helen M. I. Osborn ,
Francesca Greco
This paper is made freely available by the publisher.
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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.