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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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Publication details

The article was received on 15 Aug 2016, accepted on 21 Oct 2016 and first published on 15 Nov 2016


Article type: Communication
DOI: 10.1039/C6PY01418F
Citation: Polym. Chem., 2016,7, 7204-7210
  • Open access: Creative Commons BY license
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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

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