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Published on: August 9, 2022
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Fatty acids for controlled release applications: A comparison between prilling and solid lipid extrusion as
A Vervaeck1, T Monteyne2, F Siepmann3
1Laboratory of Pharmaceutical Technology, Ghent University, Ghent, Belgium.
Summary
Prilling and solid lipid extrusion of fatty acid formulations containing metoprolol tartrate showed distinct drug states and release profiles. Extrusion offered better drug stability at 40°C compared to prilling.
Area of Science:
- Pharmaceutical Technology
- Materials Science
- Drug Delivery Systems
Background:
- Fatty acid-based formulations are explored for controlled drug release.
- Metoprolol tartrate (MPT) is a model drug used in these studies.
- Prilling and solid lipid extrusion (SLE) are key processing techniques.
Purpose of the Study:
- To compare solid-state characteristics, drug release, and stability of MPT in fatty acid matrices processed by prilling and SLE.
- To investigate the impact of different fatty acids (myristic, stearic, behenic) and their combinations on formulation properties.
- To analyze drug-matrix interactions and structural changes induced by each processing method.
Main Methods:
- Formulation of MPT with myristic acid, stearic acid, and behenic acid.
- Processing of formulations using prilling and solid lipid extrusion (SLE).
- Solid-state characterization, drug release studies, mathematical modeling, and stability testing at 25°C and 40°C.
Main Results:
- Prilling led to complete MPT dissolution and semi-crystalline drug formation with hydrogen bonding, while SLE resulted in crystalline MPT due to limited fatty acid melting.
- Mixed fatty acid systems exhibited lower porosity and slower drug release compared to binary systems.
- SLE-processed systems showed better storage stability at 40°C than prilled systems, with slower drug release from extrudates.
Conclusions:
- Processing method significantly influences the solid-state properties and drug release behavior of fatty acid-based MPT formulations.
- Solid lipid extrusion is a promising technique for enhancing the stability of metoprolol tartrate in fatty acid matrices.
- The composition of fatty acid mixtures affects matrix porosity and drug release kinetics, with implications for formulation design.
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