Drug release from alpha,beta-poly(N-2-hydroxyethyl)-DL-aspartamide-based microparticles

Biomaterials. 2004 Aug;25(18):4333-43. doi: 10.1016/j.biomaterials.2003.11.015.

Abstract

Spherical pH-sensitive microparticles have been prepared by reverse phase suspension polymerization technique. Starting polymer has been alpha,beta-poly(N-2-hydroxyethyl)-DL-aspartamide (PHEA) partially derivatized with glycidylmethacrylate (GMA). PHEA-GMA copolymer (PHG) has been crosslinked in the presence of acrylic acid (AA) or methacrylic acid (MA) at various concentration. The obtained microparticles have been characterized by FT-IR spectrophotometry, particle size distribution analysis and scanning electron microscopy. In order to have information about water affinity of the prepared samples, swelling measurements have been carried out in aqueous media which simulate some biological fluids. The possibility to employ the prepared samples as pH-sensitive microparticles has been investigated by performing in vitro release studies. Experimental data have showed that the release rate from these microparticles depends on the environmental pH and the chemical structure of the drug.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Absorption
  • Body Fluids / chemistry*
  • Delayed-Action Preparations / administration & dosage*
  • Delayed-Action Preparations / chemistry*
  • Diffusion
  • Drug Carriers / administration & dosage
  • Drug Carriers / chemistry
  • Drug Delivery Systems / methods
  • Drug Evaluation, Preclinical
  • Hydrogels / administration & dosage
  • Hydrogels / chemistry
  • Microspheres
  • Molecular Conformation
  • Particle Size
  • Peptides / administration & dosage*
  • Peptides / chemistry*
  • Pharmaceutical Preparations / administration & dosage*
  • Pharmaceutical Preparations / chemistry*
  • Water / chemistry

Substances

  • Delayed-Action Preparations
  • Drug Carriers
  • Hydrogels
  • Peptides
  • Pharmaceutical Preparations
  • alpha,beta-poly((2-hydroxyethyl)-aspartamide)
  • Water