Investigating the Dissolution Performance of Amorphous Solid Dispersions Using Magnetic Resonance Imaging and Proton...

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Poorly water-soluble drugs pose bioavailability challenges.
• Amorphous solid dispersions (ASDs) enhance drug solubility and dissolution.
• Kollidon VA64 is a common polymer for ASD formulation.

Purpose of the Study:

• To investigate the dissolution performance of bicalutamide-Kollidon VA64 ASDs.
• To evaluate the impact of drug loading (5% vs. 30%) on dissolution.
• To characterize drug and polymer release mechanisms.

Main Methods:

• Fabrication of amorphous solid dispersions with varying bicalutamide loading.
• Utilized integrated magnetic resonance imaging (MRI) UV-Vis flow cell system.
• Employed off-line proton nuclear magnetic resonance (1H-NMR) spectroscopy for simultaneous drug and polymer analysis.

Main Results:

• The 5% bicalutamide loading ASD exhibited linear erosion and simultaneous release of drug and polymer.
• The 30% bicalutamide loading ASD showed slower water ingress.
• A slower dissolution rate for both bicalutamide and Kollidon VA64 was observed at 30% loading.

Conclusions:

• Drug loading significantly influences the dissolution behavior of bicalutamide ASDs.
• Lower drug loading promotes faster and more uniform drug and polymer release.
• ASD formulation strategies require careful optimization of drug loading for desired release profiles.