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Pharmaceutical Research

, Volume 32, Issue 8, pp 2775–2786 | Cite as

The Development of Direct Extrusion-Injection Moulded Zein Matrices as Novel Oral Controlled Drug Delivery Systems

  • Jacob Bouman
  • Peter Belton
  • Paul Venema
  • Erik van der Linden
  • Renko de Vries
  • Sheng QiEmail author
Research Paper

Abstract

Purpose

To evaluate the potential of zein as a sole excipient for controlled release formulations prepared by hot melt extrusion.

Methods

Physical mixtures of zein, water and crystalline paracetamol were hot melt extruded (HME) at 80°C and injection moulded (IM) into caplet forms. HME-IM Caplets were characterised using differential scanning calorimetry, ATR-FTIR spectroscopy, scanning electron microscopy and powder X-ray diffraction. Hydration and drug release kinetics of the caplets were investigated and fitted to a diffusion model.

Results

For the formulations with lower drug loadings, the drug was found to be in the non-crystalline state, while for the ones with higher drug loadings paracetamol is mostly crystalline. Release was found to be largely independent of drug loading but strongly dependent upon device dimensions, and predominately governed by a Fickian diffusion mechanism, while the hydration kinetics shows the features of Case II diffusion.

Conclusions

In this study a prototype controlled release caplet formulation using zein as the sole excipient was successfully prepared using direct HME-IM processing. The results demonstrated the unique advantage of the hot melt extruded zein formulations on the tuneability of drug release rate by alternating the device dimensions.

KEY WORDS

controlled release diffusion mechanism dissolution kinetics modelling hot melt extrusion-injection moulding Zein 

Abbreviations

ATR-FTIR

Attenuated Total Reflection Fourier Transform Infrared Spectroscopy

DSC

Differential Scanning Calorimetry

HME

Hot melt extrusion

HME-IM

Hot melt extrusion-injection moulding

IM

Injection moulding

PXRD

Powder X-ray diffraction

RH

Relative humidity

SEM

Scanning electron microscopy

Tg

Glass transition temperature

Notes

ACKNOWLEDGMENTS AND DISCLOSURES

This work is part of the Industrial Partnership Programme (IPP) Bio(-Related)Materials of the Stichting voor Fundamenteel Onderzoek der Materie (FOM), which is financially supported by the Nederlandse Organisatie voor Wetenschappelijk Onderzoek (NWO). The IPP BRM is co-financed by the Top Institute Food and Nutrition and the Dutch Polymer Institute.

Supplementary material

11095_2015_1663_MOESM1_ESM.docx (64 kb)
ESM (DOCX 64.0 kb)

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Copyright information

© Springer Science+Business Media New York 2015

Authors and Affiliations

  • Jacob Bouman
    • 1
    • 2
    • 3
  • Peter Belton
    • 4
  • Paul Venema
    • 2
  • Erik van der Linden
    • 2
  • Renko de Vries
    • 1
    • 5
  • Sheng Qi
    • 3
    Email author
  1. 1.Laboratory of Physical Chemistry and Colloid ScienceWageningen UniversityWageningenThe Netherlands
  2. 2.Laboratory of Physical Chemistry and Physics of FoodsWageningen UniversityWageningenThe Netherlands
  3. 3.School of PharmacyUniversity of East AngliaNorwichUK
  4. 4.School of ChemistryUniversity of East AngliaNorwichUK
  5. 5.Department of Biomedical EngineeringUniversity of Groningen and University Medical Centre GroningenGroningenThe Netherlands

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