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

Tools

Alshafiee, Maen and Aljammal, Mohammad K. and Markl, Daniel and Ward, Adam and Walton, Karl and Blunt, Liam and Korde, Sachin and Pagire, Sudhir K. and Kelly, Adrian L. and Paradkar, Anant and Conway, Barbara R. and Asare-Addo, Kofi (2019) Hot-melt extrusion process impact on polymer choice of glyburide solid dispersions : the effect of wettability and dissolution. International Journal of Pharmaceutics, 559. pp. 245-254. ISSN 1873-3476 (https://doi.org/10.1016/j.ijpharm.2019.01.038)

[thumbnail of Alshafiee-etal-IJP-2019-Hot-melt-extrusion-process-impact-on-polymer-choice-of-glyburide]
Preview
 Text. Filename: Alshafiee_etal_IJP_2019_Hot_melt_extrusion_process_impact_on_polymer_choice_of_glyburide.pdf
Accepted Author Manuscript
License: Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 logo
Download (732kB)| Preview

Abstract

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.

ORCID iDs

Alshafiee, Maen, Aljammal, Mohammad K., Markl, Daniel ORCID logoORCID: https://orcid.org/0000-0003-0411-733X, Ward, Adam, Walton, Karl, Blunt, Liam, Korde, Sachin, Pagire, Sudhir K., Kelly, Adrian L., Paradkar, Anant, Conway, Barbara R. and Asare-Addo, Kofi;
CORE (COnnecting REpositories)