A novel PEG–haloperidol conjugate with a non-degradable linker shows the feasibility of using polymer–drug conjugates in a non-prodrug fashion
Heath, F., Newman, A., Clementi, C., Pasut, G., Lin, H., Stephens, G. J.
It is advisable to refer to the publisher's version if you intend to cite from this work. See Guidance on citing. To link to this item DOI: 10.1039/c6py01418f Abstract/SummaryA 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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