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Enhancing Solubility of a BCS Class II Drug- Itraconazole by Developing and Optimizing Solid Lipid Nanoparticles
Irfan A Mohammed1, Sriramakamal Jonnalagadda1
1Department of Pharmaceutical Sciences, Philadelphia College of Pharmacy, Saint Joseph University, Philadelphia, PA, USA.
Pharmaceutical Nanotechnology
|January 23, 2025
Summary
This study developed itraconazole-loaded solid lipid nanoparticles (ICZ-SLNs) to enhance oral bioavailability and create an extended-release profile for treating fungal infections. The optimized ICZ-SLNs demonstrated improved physicochemical properties and stability.
Area of Science:
- Pharmaceutical Sciences
- Nanotechnology
- Drug Delivery Systems
Background:
- Itraconazole (ICZ) is an FDA-approved antifungal medication for blastomycosis, histoplasmosis, and aspergillosis.
- ICZ is a BCS Class II drug with low solubility and high permeability, resulting in poor oral bioavailability affected by food and pH.
Purpose of the Study:
- To develop, optimize, and characterize itraconazole-loaded solid lipid nanoparticles (ICZ-SLNs).
- To improve ICZ solubility and achieve an extended-release profile for enhanced therapeutic outcomes.
Main Methods:
- Utilized Central Composite Design for optimization of ICZ-SLNs.
- Evaluated physicochemical characteristics, including particle size, zeta potential, drug content, and entrapment efficiency.
- Assessed in-vitro release, differential scanning calorimetry (DSC), transmission electron microscopy (TEM), and stability.
Main Results:
- Optimized ICZ-SLNs exhibited a particle size of 335.6±8.0 nm, zeta potential of -23.8±0.5 mV, and high entrapment efficiency (99.5±1.5%).
- Demonstrated extended-release profiles over 24 hours and confirmed amorphous drug form within the nanoparticle matrix.
- TEM revealed spherical nanoparticles, and the formulation showed good stability under tested conditions.
Conclusions:
- Developed ICZ-SLNs offer a promising approach for improving oral bioavailability.
- This formulation has the potential for better therapeutic efficacy in treating systemic fungal infections.
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