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.

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Heath, F., Newman, A., Clementi, C., Pasut, G., Lin, H., Stephens, G. J., … Greco, F. (2016). A novel PEG-haloperidol conjugate with a non-degradable linker shows the feasibility of using polymer-drug conjugates in a non-prodrug fashion. Polymer Chemistry, 7(47), 7204–7210. https://doi.org/10.1039/c6py01418f

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