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Formulation and Characterization of Bioactive Agent Containing Nanodisks
Published on: March 17, 2023
Lipid Systems for the Delivery of Amphotericin B in Antifungal Therapy
Célia Faustino1, Lídia Pinheiro1
1Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649-003 Lisboa, Portugal.
Abstract:
Amphotericin B (AmB), a broad-spectrum polyene antibiotic in the clinic for more than fifty years, remains the gold standard in the treatment of life-threatening invasive fungal infections and visceral leishmaniasis. Due to its poor water solubility and membrane permeability, AmB is conventionally formulated with deoxycholate as a micellar suspension for intravenous administration, but severe infusion-related side effects and nephrotoxicity hamper its therapeutic potential. Lipid-based formulations, such as liposomal AmB, have been developed which significantly reduce the toxic side effects of the drug. However, their high cost and the need for parenteral administration limit their widespread use. Therefore, delivery systems that can retain or even enhance antimicrobial efficacy while simultaneously reducing AmB adverse events are an active area of research. Among those, lipid systems have been extensively investigated due to the high affinity of AmB for binding lipids. The development of a safe and cost-effective oral formulation able to improve drug accessibility would be a major breakthrough, and several lipid systems for the oral delivery of AmB are currently under development. This review summarizes recent advances in lipid-based systems for targeted delivery of AmB focusing on non-parenteral nanoparticulate formulations mainly investigated over the last five years and highlighting those that are currently in clinical trials.
Insights
Researchers are developing novel lipid-based delivery systems for Amphotericin B (AmB) to improve its effectiveness and reduce side effects. These advanced formulations aim for better drug accessibility, potentially through oral administration, offering a breakthrough in treating serious fungal infections.
Area of Science:
- Pharmacology
- Drug Delivery Systems
- Nanotechnology
Background:
- Amphotericin B (AmB) is a critical antifungal and antileishmanial drug but faces limitations due to poor solubility and toxicity.
- Conventional formulations cause severe side effects and nephrotoxicity, while liposomal versions are costly and require injection.
- There is a significant need for safer, more accessible Amphotericin B formulations.
Purpose of the Study:
- To review recent advancements in lipid-based delivery systems for Amphotericin B.
- To focus on non-parenteral, nanoparticulate formulations developed in the last five years.
- To highlight promising lipid systems currently in clinical trials.
Main Methods:
- Literature review of recent scientific publications and clinical trial data.
- Focus on lipid-based nanoparticulate systems for Amphotericin B delivery.
- Analysis of formulations targeting improved efficacy and reduced toxicity.
Main Results:
- Lipid systems show high affinity for Amphotericin B, enabling targeted delivery.
- Non-parenteral formulations, particularly nanoparticulate ones, are under active investigation.
- Several novel lipid-based systems are progressing towards or are in clinical trials.
Conclusions:
- Lipid-based systems offer a promising strategy to overcome Amphotericin B's limitations.
- Development of safe, cost-effective oral formulations is a key goal.
- Continued research in this area could lead to improved treatment options for invasive fungal infections and leishmaniasis.
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