Poly(2-ethyl-2-oxazoline) Conjugates with Salicylic Acid via Degradable Modular Ester Linkages

Conjugation of drugs to polymers is a widely used approach to gain control over the release of therapeutics. In this contribution, salicylic acid, a multipurpose model drug, is conjugated to the biocompatible poly­(2-ethyl-2-oxazoline) (PEtOx). The drug is attached to the side chains of a polymer ca...

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Bibliographic Details
Published in:Biomacromolecules 2020-08, Vol.21 (8), p.3207-3215
Main Authors: Bernhard, Yann, Sedlacek, Ondrej, Van Guyse, Joachim F. R, Bender, Johan, Zhong, Zifu, De Geest, Bruno G, Hoogenboom, Richard
Format: Article
Language:English
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Chemical Sciences
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Summary:Conjugation of drugs to polymers is a widely used approach to gain control over the release of therapeutics. In this contribution, salicylic acid, a multipurpose model drug, is conjugated to the biocompatible poly­(2-ethyl-2-oxazoline) (PEtOx). The drug is attached to the side chains of a polymer carrier through a hydrolytically cleavable ester linker, via a sequential postpolymerization modification. The chemical modulation of this ester, i.e., by primary or secondary alcohols, is demonstrated to greatly influence the ester hydrolysis rate. This crucial parameter allows us to tune the in vitro kinetics of the sustained drug release for periods exceeding a month in phosphate-buffered saline (PBS). The synthetic accessibility of the cleavable linker, together with the modularity of the drug release rate offered by this approach, highlights the utility of this class of polymers in the field of long-lasting drug delivery systems for persistent and chronic disease treatment.
ISSN:1525-7797
1526-4602
DOI:10.1021/acs.biomac.0c00659