Factors That Influence Sustained Release from Hot-Melt Extrudates

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Materials Science

Background:

• Hot-melt extrusion (HME) is a pharmaceutical manufacturing technique.
• HME is primarily used to enhance the solubility of poorly soluble drugs.
• Its application in creating sustained-release formulations is less common but holds potential.

Purpose of the Study:

• To investigate the impact of polymer selection, drug loading, milling, and hydrodynamics on flurbiprofen release from HME sustained-release formulations.
• To identify key factors influencing drug release kinetics from Eudragit-based extrudates.

Main Methods:

• Hot-melt extrusion of flurbiprofen with Eudragit polymers (RL and RS).
• Controlled milling of extrudates to achieve varying particle sizes (<125 µm to 2 mm threads).
• In vitro dissolution testing under different hydrodynamic conditions to assess drug release profiles.

Main Results:

• Polymer choice (Eudragit RL vs. RS) and particle size reduction significantly affected flurbiprofen release rates.
• Eudragit RL extrudates showed higher release (up to 84% in 12h) with smaller particle sizes (<125 µm) compared to Eudragit RS (up to 62%).
• Drug loading and hydrodynamic conditions had minimal impact on the release profile, indicating formulation robustness.

Conclusions:

• Hot-melt extrusion allows for precise control over drug release profiles through strategic selection of polymers and particle size.
• This technique offers a robust method for developing tailored sustained-release formulations adaptable to various therapeutic needs.
• HME provides a versatile platform for optimizing drug delivery by manipulating formulation parameters.