Hot-melt extrusion process impact on polymer choice of glyburide solid dispersions: The effect of wettability and dissolution

[Display omitted] •Solid dispersions of glyburide made by hot-melt extrusion.•SEM and focus variation showed microstructure and surface morphology was significantly different.•XµT showed that an increase in polymer content brought about a decrease in porosity.•Static and dynamic contact angle correl...

Full description

Saved in:
Bibliographic Details
Published in:International journal of pharmaceutics 2019-03, Vol.559, p.245-254
Main Authors: Alshafiee, Maen, Aljammal, Mohammad K., Markl, Daniel, Ward, Adam, Walton, Karl, Blunt, Liam, Korde, Sachin, Pagire, Sudhir K., Kelly, Adrian L., Paradkar, Anant, Conway, Barbara R., Asare-Addo, Kofi
Format: Article
Language:English
Subjects:
Contact angle
Glyburide
Hot-melt extrusion
Kollidon® VA64
Solid dispersion
Soluplus
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:[Display omitted] •Solid dispersions of glyburide made by hot-melt extrusion.•SEM and focus variation showed microstructure and surface morphology was significantly different.•XµT showed that an increase in polymer content brought about a decrease in porosity.•Static and dynamic contact angle correlated with dissolution using FASSIF media.•Liquid imbibition captured by dynamic contact angle affects dissolution performance. The aim of this study was to evaluate the choice of polymer and polymer level on the performance of the microstructure and wettability of hot-melt extruded solid dispersion of Glyburide (Gly) as a model drug. The produced solid dispersion were characterised using scanning electron microscopy (SEM), image analysis using a focus variation instrument (FVI), differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), X-ray microtomography (XµT), dynamic contact angle measurement and dissolution analysis using biorelevant dissolution media (FASSIF). SEM and focus variation analysis showed that the microstructure and surface morphology was significantly different between samples produced. This was confirmed by further analysis using XµT which showed that an increase in polymer content brought about a decrease in the porosity of the hot-melt extruded dispersions. DSC suggested complete amorphorisation of Gly whereas XRPD suggested incomplete amorphorisation. The static and dynamic contact angle measurement correlated with the dissolution studies using FASSIF media indicating that the initial liquid imbibition process as captured by the dynamic contact angle directly affects the dissolution performance.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2019.01.038