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

22 Citations (Scopus)

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.
LanguageEnglish
Pages175-185
Number of pages11
JournalInternational Journal of Pharmaceutics
Volume499
Issue number1-2
Early online date6 Jan 2016
DOIs
Publication statusPublished - 29 Feb 2016

Fingerprint

Albendazole
Powder Diffraction
Differential Scanning Calorimetry
X-Ray Diffraction
Electron Scanning Microscopy
Pharmaceutical Preparations
Povidone
X Ray Computed Tomography
Dosage Forms
Therapeutic Uses
Solubility
Biological Availability
Polymers
Tomography
Water
Research

Keywords

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

Cite this

Martinez Marcos, Laura ; Lamprou, Dimitrios ; McBurney, Roy ; Halbert, Gavin. / A novel hot-melt extrusion formulation of albendazole for increasing dissolution properties. In: International Journal of Pharmaceutics. 2016 ; Vol. 499, No. 1-2. pp. 175-185.
@article{46bf631fcc3049168518c93b1e374095,
title = "A novel hot-melt extrusion formulation of albendazole for increasing dissolution properties",
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.",
keywords = "hot-melt extrusion, amorphous solid dispersions, albendazole, continuous manufacturing, µ-CT",
author = "{Martinez Marcos}, Laura and Dimitrios Lamprou and Roy McBurney and Gavin Halbert",
note = "Copyright {\circledC} 2016 Elsevier B.V. All rights reserved.",
year = "2016",
month = "2",
day = "29",
doi = "10.1016/j.ijpharm.2016.01.006",
language = "English",
volume = "499",
pages = "175--185",
journal = "International Journal of Pharmaceutics",
issn = "0378-5173",
number = "1-2",

}

A novel hot-melt extrusion formulation of albendazole for increasing dissolution properties. / Martinez Marcos, Laura; Lamprou, Dimitrios; McBurney, Roy; Halbert, Gavin.

In: International Journal of Pharmaceutics, Vol. 499, No. 1-2, 29.02.2016, p. 175-185.

Research output: Contribution to journalArticle

TY - JOUR

T1 - A novel hot-melt extrusion formulation of albendazole for increasing dissolution properties

AU - Martinez Marcos, Laura

AU - Lamprou, Dimitrios

AU - McBurney, Roy

AU - Halbert, Gavin

N1 - Copyright © 2016 Elsevier B.V. All rights reserved.

PY - 2016/2/29

Y1 - 2016/2/29

N2 - 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.

AB - 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.

KW - hot-melt extrusion

KW - amorphous solid dispersions

KW - albendazole

KW - continuous manufacturing

KW - µ-CT

UR - http://www.scopus.com/inward/record.url?scp=84954116442&partnerID=8YFLogxK

UR - http://www.sciencedirect.com/science/article/pii/S0378517316300059

U2 - 10.1016/j.ijpharm.2016.01.006

DO - 10.1016/j.ijpharm.2016.01.006

M3 - Article

VL - 499

SP - 175

EP - 185

JO - International Journal of Pharmaceutics

T2 - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-2

ER -