Topical Amphotericin B solid lipid nanoparticles: Design and development.

Area of Science:

• Pharmaceutical Sciences
• Nanotechnology
• Dermatology

Background:

• Amphotericin B is a potent antifungal agent with limited topical efficacy due to poor solubility and skin penetration.
• Development of effective topical drug delivery systems is crucial for treating fungal skin infections.

Purpose of the Study:

• To design and develop topical Amphotericin B-loaded solid lipid nanoparticles (SLNs).
• To enhance the therapeutic antifungal activity of Amphotericin B through improved topical delivery.

Main Methods:

• Amphotericin B SLNs were prepared using a novel solvent diffusion method.
• Characterization included particle size, zeta potential, drug entrapment, surface morphology, in vitro antifungal activity, ex vivo permeation, retention, and skin-irritation studies.
• Stability was assessed through lyophilization with and without cryoprotectants.

Main Results:

• Optimized SLNs were spherical (111.1±2.2nm) with high drug entrapment (93.8±1.8%) and a negative zeta potential (-23.98±1.36mV).
• No drug-lipid interactions were observed; Amphotericin B was well dispersed within the lipid matrix.
• Optimized SLN formulation showed a 2-fold increase in ex vivo drug permeation and enhanced antifungal activity against Trichophyton rubrum compared to plain drug dispersion.
• SLN formulations lyophilized without cryoprotectants showed increased particle size, indicating the importance of cryoprotectants for stability.

Conclusions:

• Solid lipid nanoparticles are effective carriers for poorly water-soluble drugs like Amphotericin B.
• Topical Amphotericin B SLNs significantly enhance antifungal efficacy and skin permeation, offering a promising approach for treating fungal infections.
• The developed SLN formulation demonstrated good stability at refrigerated and room temperatures for three months.