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

Abstract

The objective of this study was to develop a floating, pulsatile, multiparticulate drug delivery system intended for chronopharmacotherapy of arthritis. The floating pulsatile drug delivery has the advantage that a drug can be released in the upper gastrointestinal tract after a definite time period of no drug release, i.e. lag time. Cross-linked beads were prepared using low methoxylated pectin (LM104AS), sodium alginate, and low methoxylated pectin (LM104AS) along with sodium alginate by acid- base reaction during ionotropic gelation. Beads were dried in oven at 50°C for 4 h. Aceclofenac was used as a model drug for encapsulation. Drug loaded multiparticulates were subjected to various characterization and evaluation parameters like entrapment efficiency, surface topography, size analysis and in vitro release study. It was found that calcium pectinate beads show maximum drug entrapment. Hence, pectin containing formulation was further studied for buoyancy, DSC and radio imaging study. Drug release study was performed in acidic environment using pH 1.2 buffer solution for 6 h and then at 7.4 pH for 60 min. The total drug release ranges from 5–10% and 90–94% in acidic and basic media, respectively.

Keywords::

• Floating pulsatile
• multiparticulates
• release kinetics
• radio imaging
• chronopharmacotherapy

Acknowledgments

The authors are grateful to Department of Physics, Pune, India, for providing the facility of SEM, C P Kelco, Mumbai, India, for providing the pectin and Alembic Laboratories Ltd, Vadodara, for providing gift sample of aceclofenac.

Declaration of interest: The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the paper.