Studies on mefenamic acid microparticles: formulation, in vitro release, and in situ studies in rats

AAPS PharmSciTech. 2009;10(1):104-12. doi: 10.1208/s12249-008-9183-0. Epub 2009 Jan 29.

Abstract

In this study, we investigated the in vitro characteristics of mefenamic acid (MA) microparticles as well as their effects on DNA damage. MA-loaded chitosan and alginate beads were prepared by the ionotropic gelation process. Microsponges containing MA and Eudragit RS 100 were prepared by quasi-emulsion solvent diffusion method. The microparticles were characterized in terms of particle size, surface morphology, encapsulation efficiency, and in vitro release profiles. Most of the formulation variables manifested an influence on the physical characteristics of the microparticles at varying degrees. We also studied the effects of MA, MA-loaded microparticles, and three different polymers on rat brain cortex DNA damage. Our results showed that DNA damage was higher in MA-loaded Eudragit microsponges than MA-loaded biodegradable chitosan or alginate microparticles.

MeSH terms

  • Acrylic Resins / chemistry
  • Alginates / chemistry
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Cerebral Cortex / drug effects*
  • Cerebral Cortex / pathology
  • Chemistry, Pharmaceutical
  • Chitosan / chemistry
  • DNA Damage*
  • Dosage Forms
  • Drug Carriers
  • Drug Compounding
  • Excitatory Amino Acid Agonists / toxicity
  • Glucuronic Acid / chemistry
  • Hexuronic Acids / chemistry
  • Kainic Acid / toxicity
  • Kinetics
  • Mefenamic Acid / chemistry
  • Mefenamic Acid / pharmacology*
  • Neuroprotective Agents / chemistry
  • Neuroprotective Agents / pharmacology*
  • Particle Size
  • Rats
  • Rats, Sprague-Dawley
  • Solubility
  • Technology, Pharmaceutical / methods

Substances

  • Acrylic Resins
  • Alginates
  • Anti-Inflammatory Agents, Non-Steroidal
  • Dosage Forms
  • Drug Carriers
  • Excitatory Amino Acid Agonists
  • Hexuronic Acids
  • Neuroprotective Agents
  • Eudragit RS
  • Mefenamic Acid
  • Glucuronic Acid
  • Chitosan
  • Kainic Acid