Amphiphilic association systems for Amphotericin B delivery

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Drug Delivery Systems

Background:

• Amphotericin B (AMB) is a vital antifungal agent with limited solubility.
• Developing effective drug delivery systems is crucial for enhancing AMB's therapeutic index.
• Amphiphilic association systems offer potential for solubilizing poorly soluble drugs.

Purpose of the Study:

• To produce and characterize novel amphiphilic association systems for Amphotericin B (AMB).
• To evaluate the impact of these systems on AMB solubility, stability, and diffusion.
• To assess the potential of microemulsions and monoglyceride-water systems for AMB drug formulation.

Main Methods:

• Production and characterization of three microemulsion classes and monoglyceride-water systems.
• Assessment of macroscopic properties, pH, rheology, mean size, and size distribution.
• Quantification of AMB solubility and stability using High-Performance Liquid Chromatography (HPLC).
• In vitro diffusion studies using a Franz cell system with nylon membranes.

Main Results:

• Formulations increased AMB solubility up to 20-fold compared to individual phases.
• AMB-loaded systems demonstrated good physical stability (no phase separation) for up to three months.
• Chemical stability was maintained, with unchanged AMB content in some formulations after three months.
• Diffusion studies indicated controlled release characteristics from model microemulsions.

Conclusions:

• Amphiphilic association systems, including microemulsions and monoglyceride-water systems, are effective in enhancing AMB solubility.
• These systems exhibit favorable physical and chemical stability, crucial for pharmaceutical applications.
• The developed formulations show promise for improving the delivery and efficacy of Amphotericin B.