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Encochleated Amphotericin B: Is the Oral Availability of Amphotericin B Finally Reached?
Maria Aigner1, Cornelia Lass-Flörl1
1Institute of Hygiene and Medical Microbiology, Medical University of Innsbruck, Schöpfstraße 41, Innsbruck A-6020, Austria.
Abstract:
As the oldest and for many decades the only available agent for the treatment of life-threatening invasive fungal diseases, amphotericin B (AmB) is known for its broad-spectrum fungicidal activity against a wide range of yeasts and molds. However, the main drawback of the present formulations remains its toxicity, the limited use to intravenous administration, and the higher costs associated with the better tolerated lipid formulations. The novel nanoparticle-based encochleated AmB (CAmB) formulation encapsulates, protects, and delivers its cargo molecule AmB in the interior of a calcium-phospholipid anhydrous crystal. Protecting AmB from harsh environmental conditions and gastrointestinal degradation, CAmB offers oral availability in conjunction with reduced toxicity. Matinas BioPharma, Bedminster, NJ is on the way to develop CAmB named MAT2203, currently undergoing Phase II clinical trials.
Insights
A new oral formulation of amphotericin B (AmB), known as encochleated AmB (CAmB), shows promise for treating invasive fungal infections. This novel delivery method reduces toxicity and offers oral availability, improving upon traditional intravenous treatments.
Area of Science:
- Mycology
- Pharmacology
- Nanotechnology
Background:
- Amphotericin B (AmB) is a critical antifungal agent but suffers from toxicity and limited administration routes.
- Current lipid formulations improve tolerability but increase costs and remain intravenous.
- Invasive fungal diseases require effective and safer treatment options.
Purpose of the Study:
- To introduce and evaluate a novel nanoparticle-based formulation of AmB, encochleated AmB (CAmB).
- To assess the potential of CAmB for oral administration and reduced toxicity.
- To highlight the development of CAmB (MAT2203) in ongoing clinical trials.
Main Methods:
- Development of a nanoparticle formulation encapsulating AmB within a calcium-phospholipid anhydrous crystal.
- Protection of AmB from degradation using the encochleated structure.
- Evaluation of oral bioavailability and toxicity profiles.
Main Results:
- CAmB protects amphotericin B from gastrointestinal degradation.
- The formulation enables oral availability of AmB.
- Reduced toxicity is anticipated compared to conventional AmB formulations.
Conclusions:
- Encocleated AmB (CAmB) represents a significant advancement in antifungal drug delivery.
- This novel formulation offers a potentially safer and more convenient oral treatment option for invasive fungal diseases.
- Further clinical evaluation of CAmB (MAT2203) is warranted.
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