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

Ferhan Sevgi1, Aysu Yurdasiper, Buket Kaynarsoy

  • 1Department of Pharmaceutical Technology, Faculty of Pharmacy, Ege University, 35100, Bornova, Izmir, Turkey, ferhan.sevgi@ege.edu.tr.

AAPS Pharmscitech
|February 3, 2009
PubMed

Insights

Mefenamic acid (MA) microparticles were developed using chitosan, alginate, and Eudragit RS 100. Eudragit microsponges showed higher DNA damage compared to chitosan or alginate microparticles.

Area of Science:

  • Pharmacology
  • Materials Science
  • Biotechnology

Background:

  • Mefenamic acid (MA) is a non-steroidal anti-inflammatory drug.
  • Drug delivery systems aim to improve therapeutic efficacy and reduce side effects.
  • Microparticles offer potential for controlled drug release and targeted delivery.

Purpose of the Study:

  • To prepare and characterize mefenamic acid (MA)-loaded microparticles using chitosan, alginate, and Eudragit RS 100.
  • To evaluate the in vitro characteristics, including particle size, morphology, encapsulation efficiency, and release profiles.
  • To assess the effects of MA and its loaded microparticles on rat brain cortex DNA damage.

Main Methods:

  • MA-loaded chitosan and alginate beads were synthesized via ionotropic gelation.
  • MA-loaded Eudragit RS 100 microsponges were prepared using the quasi-emulsion solvent diffusion method.
  • Microparticle characterization involved particle size analysis, surface morphology (SEM), encapsulation efficiency determination, and in vitro drug release studies.
  • DNA damage assay was performed on rat brain cortex samples.

Main Results:

  • Formulation variables significantly influenced the physical characteristics and in vitro release of MA microparticles.
  • MA-loaded Eudragit RS 100 microsponges exhibited higher levels of rat brain cortex DNA damage compared to MA-loaded chitosan or alginate microparticles.
  • The study demonstrated varying degrees of polymer influence on microparticle properties and biological effects.

Conclusions:

  • Chitosan and alginate microparticles represent potentially safer delivery systems for mefenamic acid compared to Eudragit RS 100 microsponges, particularly concerning genotoxicity.
  • The choice of polymer and preparation method significantly impacts the physicochemical properties and biological safety of mefenamic acid microparticles.
  • Further investigation into the mechanism of DNA damage induced by Eudragit-based mefenamic acid microparticles is warranted.

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