Abstract
PurposeIn 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.MethodsCaplets 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 a zein based matrix for drug delivery.ResultsDrug 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.ConclusionThe drug state and pH dependant electrostatic interactions are hypothesised to influence release kinetics. Both factors can potentially be used to influence release kinetics release, thereby broadening the horizon for zein as a tuneable release agent.Electronic supplementary materialThe online version of this article (doi:10.1007/s11095-015-1818-8) contains supplementary material, which is available to authorized users.
Highlights
Electronic supplementary material The online version of this article contains supplementary material, which is available to authorized users.University Medical Centre Groningen, Groningen, The NetherlandsIn the field of sustained and controlled release, biopolymers are increasing in popularity as compared to synthetic polymers, since they have the advantages of being biocompatible, environmentally sustainable and often inexpensive
An example is the maize corn protein zein, which has proven to be quite promising for sustained release applications
We have recently investigated the use of zein as a hot-melt extrusion-injection moulded (HME-injection moulding (IM)) caplet excipient [6]
Summary
In the field of sustained and controlled release, biopolymers are increasing in popularity as compared to synthetic polymers, since they have the advantages of being biocompatible, environmentally sustainable and often inexpensive. An example is the maize corn protein zein, which has proven to be quite promising for sustained release applications. It has been studied for controlled release in formats such as microcapsules [1,2], fibers [3,4], films [5] and monolithic devices [6,7]. Ideal polymers for sustained release are biocompatible, nontoxic, physically, chemically and microbiologically stable and most important of all, providing a slow but tuneable release [8]
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