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Lipid-based amphotericin B formulations: from animals to man
1Fujisawa Healthcare, Inc., Three Parkway North, Deerfield, IL 60015, USA.
Abstract:
Amphotericin B has been the mainstay of systemic antifungal therapy for over 30 years, despite its serious side-effects, and, although numerous alternative antifungal agents have been developed, none to date has matched the efficacy of amphotericin B. However, modern drug delivery technology has improved the safety of amphotericin B by incorporating it into lipid-based delivery systems, including liposomes. Three such formulations, based on the natural affinity of amphotericin B for lipids, are currently marketed. All increase the therapeutic index of amphotericin B, thereby allowing more aggressive treatment than is possible with the conventional product. However, they differ in structure, side-effect profiles and evidence of proven efficacy as discussed in this review.
Insights
Amphotericin B remains a key antifungal drug, but lipid formulations significantly improve its safety and therapeutic index. This review compares these advanced delivery systems for better systemic antifungal treatment.
Area of Science:
- Mycology
- Pharmacology
- Drug Delivery Systems
Background:
- Amphotericin B has been a primary systemic antifungal agent for over three decades.
- Despite its efficacy, severe side effects limit its use.
- Newer antifungal agents have not surpassed Amphotericin B's effectiveness.
Purpose of the Study:
- To review modern lipid-based drug delivery systems for Amphotericin B.
- To compare the efficacy and safety profiles of marketed liposomal formulations.
- To highlight advancements in Amphotericin B's therapeutic index.
Main Methods:
- Review of existing literature on Amphotericin B and its lipid formulations.
- Analysis of structural differences between liposomal Amphotericin B products.
- Comparison of clinical data regarding efficacy and side effects.
Main Results:
- Lipid formulations enhance Amphotericin B's safety by reducing toxicity.
- Three marketed liposomal Amphotericin B formulations exist, differing in structure and side-effect profiles.
- These formulations allow for more aggressive treatment compared to conventional Amphotericin B.
Conclusions:
- Lipid-based drug delivery has significantly improved Amphotericin B's safety profile.
- Marketed liposomal formulations offer improved therapeutic indices.
- Understanding formulation-specific differences is crucial for optimal systemic antifungal therapy.
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