A novel hot-melt extrusion formulation of albendazole for increasing dissolution properties

Laura Martinez Marcos, Dimitrios Lamprou, Roy McBurney, Gavin Halbert

Research output: Contribution to journalArticle

32 Citations (Scopus)
201 Downloads (Pure)

Abstract

The main aim of the research focused on the production of hot-melt extrusion (HME) formulations with increased dissolution properties of albendazole (ABZ). Therefore, HME was applied as a continuous manufacturing technique to produce amorphous solid dispersions of the poorly water soluble drug ABZ combined with the polymer matrix polyvinylpyrrolidone PVP K12. HME formulations of ABZ – PVP K12 comprised a drug content of 1%, 5% and 10% w/w. The main analytical characterisation techniques used were Scanning Electron Microscopy (SEM), Micro-computed Tomography (µ-CT), X-Ray Powder Diffraction (XRPD), Differential Scanning Calorimetry (DSC) and dissolution profile studies. The application of SEM, XRPD and DSC evidenced drug physical transformation from crystalline to amorphous state and therefore, the achievement of an amorphous solid dispersion. The introduction of a novel technique, µ-CT, to characterise the internal structure of these materials revealed key information regarding materials distribution and void content. Dissolution profile studies evidenced a high increase in drug release profile compared to pure ABZ. These promising results can lead to a great enhancement of the oral bioavailability of ABZ dosage forms. Therefore, HME is a potential continuous manufacturing technique to overcome ABZ poor solubility properties and lead to a significant increase in the therapeutic effect.
Original languageEnglish
Pages (from-to)175-185
Number of pages11
JournalInternational Journal of Pharmaceutics
Volume499
Issue number1-2
Early online date6 Jan 2016
DOIs
Publication statusPublished - 29 Feb 2016

Keywords

  • hot-melt extrusion
  • amorphous solid dispersions
  • albendazole
  • continuous manufacturing
  • µ-CT

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