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Bulk Flow Optimisation of Amorphous Solid Dispersion Excipient Powders through Surface Modification
Danni Suhaidi1, Yao-Da Dong2, Paul Wynne3
1School of Engineering, Deakin University, Waurn Ponds, VIC 3216, Australia.
Pharmaceutics
|May 27, 2023
Summary
L-leucine coprocessing improves amorphous solid dispersion (ASD) powder flowability for many excipients. This study investigated L-leucine
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Chemical Engineering
Background:
- Amorphous solid dispersions (ASDs) enhance drug oral bioavailability and macromolecule stability in solid dosage forms.
- Spray-dried ASDs exhibit surface cohesion and hygroscopicity, negatively impacting powder flow and processing.
- Surface modification is crucial for improving the bulk properties of ASDs.
Purpose of the Study:
- To investigate the effectiveness of L-leucine (L-leu) coprocessing in modifying the particle surface of ASD-forming materials.
- To assess the impact of L-leu on the bulk characteristics and flowability of various prototype ASD excipients.
- To understand the mechanistic behavior of L-leu during coformulation with different polymers.
Main Methods:
- Coprocessing of L-leucine with various prototype ASD excipients including maltodextrin, polyvinylpyrrolidone (PVP K10 and K90), trehalose, gum arabic, and hydroxypropyl methylcellulose (HPMC E5LV and K100M).
- Spray-drying under controlled conditions to minimize particle size influence on cohesion.
- Morphological evaluation using scanning electron microscopy (SEM).
- Bulk powder characterization using a powder rheometer to assess flowability, flow rate sensitivity, and compactability.
Main Results:
- L-leucine coprocessing generally improved the flowability of maltodextrin, PVP K10, trehalose, and gum arabic formulations.
- Scanning electron microscopy revealed both known and novel morphological changes on the particle surfaces.
- Polyvinylpyrrolidone K90 and hydroxypropyl methylcellulose formulations presented unique challenges, offering insights into L-leucine's mechanistic behavior.
Conclusions:
- L-leucine is an effective excipient for improving the powder flow properties of certain amorphous solid dispersions.
- Further research is recommended to explore the interplay between L-leucine and the physico-chemical properties of coformulated excipients.
- Enhanced bulk characterization tools are needed to fully understand the multifactorial impact of L-leucine surface modification.
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