Preparation and Characterization of Spherical Amorphous Solid Dispersion with Amphotericin B

Area of Science:

• Pharmaceutical Technology
• Materials Science
• Drug Delivery Systems

Background:

• Amphotericin B (AmB) exhibits poor solubility and a tendency for toxic aggregation in vivo.
• Existing formulations often face challenges in achieving optimal therapeutic efficacy and safety profiles.
• Cyclodextrin polymers offer potential for improving drug properties through complexation and dispersion.

Purpose of the Study:

• To develop novel polymer microspheres of amphotericin B (AmB) using cyclodextrin polymers (Poly-CD) via spray drying.
• To enhance the solubility, dissolution rate, and stability of AmB.
• To explore the potential for oral or pulmonary administration of the developed AmB formulations.

Main Methods:

• Spray drying technique was employed to synthesize AmB-loaded Poly-CD microspheres.
• Comprehensive characterization included SEM, FT-IR, DSC, thermal analysis, and Raman spectroscopy.
• Particle size analysis, drug purity tests, and in vitro drug release studies were conducted.

Main Results:

• Spray drying successfully produced spherical amorphous solid dispersions of AmB within Poly-CD.
• Characterization confirmed the amorphous state of AmB, with its chemical structure intact.
• Optimized formulations demonstrated complete AmB release within 40 minutes in vitro.
• The amorphous solid dispersion approach prevented crystalline AmB aggregation.

Conclusions:

• The study successfully developed AmB-loaded polymer microspheres using spray-dried cyclodextrin polymers.
• The amorphous solid dispersion strategy significantly improved AmB solubility and dissolution.
• These findings suggest a promising new generation of AmB formulations for potential oral or pulmonary drug delivery, mitigating in vivo toxicity.