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Unveiling the Amphotericin B Degradation Pathway and Its Kinetics in Lipid-Based Solutions
Éverton N Alencar1, Phawanan Sawangchan2, Lee E Kirsch2
1Graduate Program in Pharmaceutical Nanotechnology, Federal University of Rio Grande do Norte (UFRN), Av. General Gustavo Cordeiro de Faria-SN-Petrópolis, Natal, Rio Grande do Norte 59012-570, Brazil; Division of Pharmaceutics and Translational Therapeutics, College of Pharmacy, The University of Iowa, 115 S. Grand Avenue, Iowa City, IA 52242, USA.
Journal of Pharmaceutical Sciences
|November 12, 2020
Summary
Amphotericin B (AmB) degradation in lipid solutions depends on storage conditions. Antioxidants and protection from light significantly improve AmB stability, suggesting optimal storage for pharmaceutical formulations.
Area of Science:
- Pharmaceutical Sciences
- Drug Stability
- Formulation Development
Background:
- Amphotericin B (AmB) is a vital antifungal agent often formulated in lipid-based systems.
- Understanding AmB degradation kinetics is crucial for ensuring therapeutic efficacy and product shelf-life.
Purpose of the Study:
- To elucidate the degradation pathways and kinetics of Amphotericin B (AmB) in various lipid-based solutions.
- To identify critical factors influencing AmB stability under different storage conditions.
Main Methods:
- Quantification of AmB using High-Performance Liquid Chromatography (HPLC) and UV-Vis spectrometry.
- Systematic evaluation of AmB stability under varying surface area, temperature, light exposure, and presence of antioxidants/co-solutes.
- Estimation of degradation rate constants via nonlinear regression analysis.
Main Results:
- HPLC method demonstrated high precision and accuracy (linearity 4.45–52.0 nM).
- Adsorption to glass surfaces did not impact AmB loss; unsaturated oils and methanol offered better AmB preservation than medium-chain triglycerides.
- Temperature nonlinearly increased AmB degradation, while antioxidants effectively reduced it. Autoxidation predominated in the dark, and photo-oxidation followed pseudo-first-order kinetics under light.
Conclusions:
- Optimal storage of AmB in oily formulations involves glass vials protected from light, supplemented with antioxidants.
- Further research into diverse media is recommended for comprehensive modeling of AmB degradation in lipid-based formulations.
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