Hot melt extruded zein for controlled delivery of diclofenac sodium: Effect of drug loading and medium composition

This study evaluates the potential use of zein as an excipient in hot-melt extrusion for controlled delivery of diclofenac sodium (DS). Mixtures of zein, polyethylene glycol and drug were hot melt extruded and cut into 2 mm extrudates. Extrudates were characterised using differential scanning calorimetry, X-ray powder diffraction and scanning electron microscopy. The drug in the extrudates was found to be in the non-crystalline state, independent of the drug loading. Moreover, the drug release from extrudates was investigated. The release was directly dependent on the drug loading: a controlled and nearly zero-order release was obtained at the lowest drug loading (12.5% w/w), whereas almost immediate release was achieved at higher drug loadings, i.e. 25% and 37.5%. The release was inversely dependent on the ionic strength of the medium. The influence of digestive enzymes on drug release was also studied. Pancreatin, but not pepsin, was found to have a significant influence on the drug release as well as on the microstructure of zein extrudates. These data therefore support the potential use of zein as excipient in hot melt extrusion for controlled release purposes. Continue to read on hot melt extruded zein for controlled delivery of diclofenac sodium

Keywords:  Zein, Hot melt extrusion, Controlled release, Solid dispersion, Amorphous, Diclofenac sodium

More information on Zein*
Zein is the main storage protein of corn and it has several industrial applications. Mainly in the last 10-15 years, zein has emerged as a potential pharmaceutical excipient with unique features. Zein is a natural, biocompatible and biodegradable material produced from renewable sources. It is insoluble, yet due to its amphiphilic nature, it has self-assembling properties, which have been exploited for the formation of micromicroparticle and nanoparticle and films. Moreover, zein can hydrate so it has been used in swellable matrices for controlled drug release. Other pharmaceutical applications of zein in oral drug delivery include its incorporation in solid dispersions of poorly soluble drugs and in colonic drug delivery systems.”

* Berardi A, Bisharat L, AlKhatib HS, Cespi M. Zein as a Pharmaceutical Excipient in Oral Solid Dosage Forms: State of the Art and Future Perspectives. AAPS Pharmscitech. 2018 Jul;19(5):2009-2022. DOI: 10.1208/s12249-018-1035-y.