Long-term controlled release of PLGA microparticles containing antidepressant mirtazapine

Pharm Dev Technol. 2016 Mar;21(2):214-21. doi: 10.3109/10837450.2014.991874. Epub 2014 Dec 11.

Abstract

The aim of the study was to prepare PLGA microparticles for prolonged release of mirtazapine by o/w solvent evaporation method and to evaluate effects of PVA concentration and organic solvent choice on microparticles characteristics (encapsulation efficiency, drug loading, burst effect, microparticle morphology). Also in vitro drug release tests were performed and the results were correlated with kinetic model equations to approximate drug release mechanism. It was found that dichloromethane provided microparticles with better qualities (encapsulation efficiency 64.2%, yield 79.7%). Interaction between organic solvent effect and effect of PVA concentration was revealed. The prepared samples released the drug for 5 days with kinetics very close to that of zero order (R(2 )= 0.9549 - 0.9816). According to the correlations, the drug was probably released by a combination of diffusion and surface erosion, enhanced by polymer swelling and chain relaxation.

Keywords: Drug release; PLGA; kinetics; solvent evaporation method.

MeSH terms

  • Antidepressive Agents / chemistry*
  • Delayed-Action Preparations / chemistry*
  • Drug Liberation
  • Kinetics
  • Lactic Acid / chemistry*
  • Methylene Chloride / chemistry
  • Mianserin / analogs & derivatives*
  • Mianserin / chemistry
  • Microspheres
  • Mirtazapine
  • Polyglycolic Acid / chemistry*
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Solvents / chemistry

Substances

  • Antidepressive Agents
  • Delayed-Action Preparations
  • Solvents
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Mianserin
  • Polyglycolic Acid
  • Lactic Acid
  • Methylene Chloride
  • Mirtazapine