A novel PEG–haloperidol conjugate with a non-degradable linker shows the feasibility of using polymer–drug conjugates in a non-prodrug fashion

文献情報

出版日 2016-11-15

DOI 10.1039/C6PY01418F

インパクトファクター 5.582

著者

Felicity Heath, Amy Newman, Chiara Clementi, Gianfranco Pasut, Hong Lin, Gary J. Stephens, Benjamin J. Whalley, Helen M. I. Osborn, Francesca Greco

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要旨

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.

掲載誌

Polymer Chemistry

CiteScore: 8.6

自己引用率: 7.3%

年間論文数: 457

Polymer Chemistry welcomes submissions in all areas of polymer science that have a strong focus on macromolecular chemistry. Manuscripts may cover a broad range of fields, yet no direct application focus is required.

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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