Controlled release from zein matrices: Interplay of drug hydrophobicity and pH

Bouman, Jacob, Belton, Peter, Venema, Paul, van der Linden, Erik, de Vries, Renko and Qi, Sheng ORCID: (2016) Controlled release from zein matrices: Interplay of drug hydrophobicity and pH. Pharmaceutical Research, 33 (3). pp. 673-685. ISSN 0724-8741

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Purpose: In earlier studies, the corn protein zein is found to be suitable as a sustained release agent, yet the range of drugs for which zein has been studied remains small. Here, zein is used as a sole excipient for drugs differing in hydrophobicity and isoelectric point: indomethacin, paracetamol and ranitidine. Methods: Caplets were prepared by hot-melt extrusion (HME) and injection moulding (IM). Each of the three model drugs were tested on two drug loadings in various dissolution media. The physical state of the drug, microstructure and hydration behaviour were investigated to build up understanding for the release behaviour from zein based matrix for drug delivery. Results: Drug crystallinity of the caplets increases with drug hydrophobicity. For ranitidine and indomethacin, swelling rates, swelling capacity and release rates were pH dependent as a consequence of the presence of charged groups on the drug molecules. Both hydration rates and release rates could be approached by existing models. Conclusion: Both the drug state as pH dependant electrostatic interactions are hypothesised to influence release kinetics. Both factors can potentially be used factors influencing release kinetics release, thereby broadening the horizon for zein as a tuneable release agent.

Item Type: Article
Additional Information: This article is distributed under the terms of the Creative Commons Attribution 4.0 International License (, which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made.
Uncontrolled Keywords: zein,extrusion-injection moulding,controlled release,dissolution kinetics modelling,diffusion mechanism
Faculty \ School: Faculty of Science > School of Pharmacy
Faculty of Science > School of Chemistry
UEA Research Groups: Faculty of Science > Research Groups > Drug Delivery and Pharmaceutical Materials (former - to 2017)
Faculty of Science > Research Groups > Biophysical Chemistry (former - to 2017)
Faculty of Science > Research Groups > Pharmaceutical Materials and Soft Matter
Depositing User: Pure Connector
Date Deposited: 05 Feb 2016 08:14
Last Modified: 22 Oct 2022 00:23
DOI: 10.1007/s11095-015-1818-8


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