Melt-Extruded Eudragit® FS-Based Granules for Colonic Drug Delivery

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Materials Science

Background:

• Developing effective colonic drug delivery systems is crucial for treating localized gastrointestinal diseases.
• Eudragit® FS is a pH-dependent polymer suitable for colon-specific drug release.
• Melt extrusion offers a continuous and efficient manufacturing process for pharmaceutical formulations.

Purpose of the Study:

• To characterize Eudragit® FS-based granules prepared by melt extrusion for colonic drug delivery.
• To evaluate the drug release profiles of model compounds from these granules.
• To identify key factors influencing drug release and compare melt extrusion with conventional methods.

Main Methods:

• Melt extrusion of drug-polymer blends (Eudragit® FS with 5-ASA, theophylline, or diclofenac sodium).
• Grinding of extrudates into granules (16-40 mesh) and subsequent capsule filling.
• Three-stage dissolution testing simulating gastrointestinal tract conditions (pH 1.2, pH 6.8, pH 7.4).

Main Results:

• Melt extrusion successfully produced Eudragit® FS granules with crystalline drug dispersion.
• Granules showed pH-dependent release, with minimal 5-ASA release at pH 1.2 and 6.8, and complete release at pH 7.4.
• Drug loading and granule size were identified as critical factors controlling 5-ASA release.

Conclusions:

• Melt extrusion is a viable process for preparing Eudragit® FS granules for colon-specific delivery of 5-ASA.
• The prepared granules exhibit desirable properties for colonic targeting, with controlled release profiles.
• Melt-extruded granules showed improved physical characteristics (lower porosity, higher strength) compared to conventionally processed granules.