Compacted Multiparticulate Systems for Colon-Specific Delivery of Ketoprofen

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Colon-specific drug delivery aims to enhance therapeutic efficacy and reduce systemic side effects.
• Pellet-containing tablets offer a promising alternative to monolithic tablets and capsules for targeted delivery.
• Understanding the impact of formulation and compaction on coated pellets is crucial for optimizing colon targeting.

Purpose of the Study:

• To evaluate the influence of formulation and compaction factors on the integrity and drug release of ketoprofen-loaded pellets within tablets.
• To compare the performance of acrylic polymers Eudragit® FS 30 D (PMMA) and Opadry® 94k28327 (PMA) in coated pellets for colon-specific delivery.
• To determine the key tablet characteristics affecting ketoprofen release and colon targeting.

Main Methods:

• Ketoprofen pellets prepared via extrusion-spheronization and coated with PMMA or PMA.
• Coated pellets mixed with placebo granules and compressed into tablets using a hydraulic press.
• Analysis of film integrity, pellet characteristics (hardness, friability, disintegration), and ketoprofen release profiles.

Main Results:

• Ketoprofen release was significantly influenced by pellet content, hardness, friability, and disintegration time.
• PMA-containing tablets showed rapid disintegration (<1 min) and drug release similar to uncompressed pellets under low compaction.
• PMMA-containing tablets exhibited higher rupture resistance, with high pellet content leading to non-disintegrating matrices.

Conclusions:

• Pellet-containing tablets can effectively target ketoprofen to the colon.
• The targeting capacity is directly dependent on the physicochemical properties of the tablets, influenced by polymer choice and compaction parameters.
• Optimized formulation and processing are essential for achieving desired drug release and colon-specific delivery.