Formulation and characterization study of itraconazole-loaded microparticles

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Materials Science

Background:

• Itraconazole is an antifungal drug with poor solubility, limiting its oral bioavailability.
• Developing effective drug delivery systems is crucial for improving itraconazole's therapeutic efficacy.
• Solvent-free methods offer environmental and safety advantages in pharmaceutical manufacturing.

Purpose of the Study:

• To develop itraconazole-loaded microparticles using a fast, simple, and solvent-free hot melt method.
• To enhance the wettability, dissolution rate, and in-vitro drug release of itraconazole.
• To evaluate the physical and technological stability of the developed microparticle formulations.

Main Methods:

• Preparation of itraconazole microparticles via a hot melt method (melting-milling-sieving).
• Characterization included drug content, particle size distribution, Differential Scanning Calorimetry (DSC), and in-vitro drug release studies.
• Physical and technological stability assessed after 12 months of storage under ambient conditions.

Main Results:

• Microparticles with diameters below 355 μm were successfully prepared.
• DSC analysis indicated that itraconazole was predominantly in an amorphous state within the microparticles.
• In-vitro drug release studies demonstrated a significantly increased release rate compared to free itraconazole.
• Formulations exhibited good physical and technological stability, with no significant changes in thermal or release profiles over 12 months.

Conclusions:

• The developed solvent-free hot melt method is effective for producing stable itraconazole microparticles.
• The microparticle formulations enhance itraconazole's dissolution rate and in-vitro drug release.
• The chosen excipients protect the amorphous form of itraconazole, ensuring consistent drug delivery performance.