Formulation and evaluation of floating, pulsatile, multiparticulates using pH-dependent swellable polymers

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Chronotherapy requires drug release timed to physiological rhythms.
• Pulsatile drug delivery systems offer controlled drug release after a specific lag time.
• Floating drug delivery systems enhance gastric residence time for improved drug absorption.

Purpose of the Study:

• To develop a floating, pulsatile, multiparticulate drug delivery system for arthritis chronotherapy.
• To utilize pectin and sodium alginate for creating cross-linked beads via ionotropic gelation.
• To encapsulate aceclofenac as a model drug for evaluating the system's performance.

Main Methods:

• Preparation of cross-linked beads using low methoxylated pectin (LM104AS) and sodium alginate.
• Ionotropic gelation employing an acid-base reaction for bead formation.
• Characterization included entrapment efficiency, surface topography, size analysis, in vitro release, buoyancy, DSC, and radio imaging.

Main Results:

• Calcium pectinate beads demonstrated maximum drug entrapment efficiency.
• Floating properties were confirmed for pectin-containing formulations.
• In vitro release studies showed 5-10% drug release in acidic media (pH 1.2) and 90-94% in basic media (pH 7.4) after specific time intervals.

Conclusions:

• The developed floating, pulsatile multiparticulate system effectively encapsulates aceclofenac.
• The system exhibits potential for chronopharmacotherapy of arthritis by providing a delayed drug release profile.
• Pectin-based formulations are suitable for creating floating, pulsatile drug delivery systems with controlled release characteristics.