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

POLYMER CHEMISTRY（2016）

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摘要

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 D-2-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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关键词

polymer–drug conjugates,peg–haloperidol conjugate,novel peg–haloperidol,non-degradable,non-prodrug

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