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Updated: May 23, 2026

Formulation and Characterization of Bioactive Agent Containing Nanodisks
Published on: March 17, 2023
[Liposomal amphotericin B: a unique pharmacokinetic profile. An unfinished story]
José Ramón Azanza Perea1, José Barberán
1José Ramón Azanza Perea, Servicio de Farmacología Clínica, Clínica Universidad de Navarra, Avenida Pío XII s/n - 31008 Pamplona, Spain. jrazanza@unav.es.
Abstract:
Amphotericin B in its lipid formulation continues to be the reference drug in the treatment of systemic fungal infections despite the time elapse since the development of this compound. The absence of fungal resistance, pharmacokinetics, and the better tolerability profile as compared with the remaining formulations of amphotericin B are sufficient reasons to justify its prominent therapeutic role. The liposome containing liposomal amphotericin B is very stable in relation to the presence of cholesterol and phospholipids are not thermolabile, so that free amphotericin B is almost inexistent (<1%), which explains the reduced incidence of effects related to the drug administration, and a reduction in the incidence of nephrotoxicity (half than that with amphotericin B lipid complex) and that even in some studies at doses of 1 mg/kg has been shown to be negligible. This profile explains the very high plasma drug concentrations and the reduced distribution volume and clearance, with a very prolonged elimination half-life. There are evidences showing that the liposome through amphotericin B is capable of binding to ergosterol present in the fungal membrane and only at this moment would be the antifungal released to exert its pharmacological effects.
Insights
Liposomal amphotericin B remains a leading treatment for systemic fungal infections due to its efficacy and improved safety profile. Its stable formulation minimizes toxicity, offering a better therapeutic option compared to other amphotericin B versions.
Area of Science:
- Mycology
- Pharmacology
- Drug Delivery Systems
Context:
- Systemic fungal infections pose significant health risks.
- Amphotericin B is a cornerstone antifungal agent.
- Liposomal formulations aim to improve drug safety and efficacy.
Purpose:
- To review the therapeutic role and characteristics of liposomal amphotericin B.
- To highlight its pharmacokinetic and safety advantages.
- To explain its mechanism of action.
Summary:
- Liposomal amphotericin B is a stable formulation with minimal free drug (<1%).
- It exhibits reduced nephrotoxicity and improved tolerability compared to other amphotericin B formulations.
- High plasma concentrations, low distribution volume, and prolonged half-life characterize its pharmacokinetics.
- The liposome targets ergosterol in fungal membranes, releasing amphotericin B for antifungal effect.
Impact:
- Liposomal amphotericin B offers a superior safety and tolerability profile for treating systemic fungal infections.
- Its pharmacokinetic properties support sustained therapeutic drug levels.
- This formulation represents a significant advancement in antifungal therapy, reducing treatment-related adverse events.
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