Swellable microparticles containing Suprofen: evaluation of in vitro release and photochemical behaviour

J Control Release. 1998 Feb 12;51(2-3):249-57. doi: 10.1016/s0168-3659(97)00177-6.

Abstract

Suprofen, an anti-inflammatory drug was incorporated in polymer networks based on biocompatible macromolecules, such as alpha,beta-polyasparthydrazide (PAHy) and alpha,beta-poly(N-hydroxyethyl)-DL-aspartamide (PHEA) crosslinked by glutaraldehyde or gamma-rays, respectively. Swelling tests carried out in aqueous media showed that pH value affects the swelling degree of the prepared hydrogels. In vitro release tests were performed in simulated gastrointestinal fluids (pH 1/6.8) using the pH variation method and in phosphate-buffered saline, pH 7.4. Experimental data indicated that Suprofen was released in a sustained way both from PAHy and PHEA microparticles. Further, incorporation of Suprofen in PAHy and PHEA networks provided a significant reduction of the drug photosensitizing activity, as evidenced by in vitro hemolysis tests.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / chemistry*
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Cross-Linking Reagents / chemistry
  • Delayed-Action Preparations
  • Erythrocytes / drug effects
  • Gastric Juice / metabolism
  • Gels
  • Glutaral / chemistry
  • Hemolysis
  • Humans
  • Hydrazines / chemistry
  • Hydrogen-Ion Concentration
  • Nylons / chemistry
  • Particle Size
  • Peptides / chemistry
  • Photosensitizing Agents / chemistry*
  • Plasma Substitutes
  • Suprofen / chemistry*
  • Suprofen / pharmacology

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Cross-Linking Reagents
  • Delayed-Action Preparations
  • Gels
  • Hydrazines
  • Nylons
  • Peptides
  • Photosensitizing Agents
  • Plasma Substitutes
  • alpha,beta-poly((2-hydroxyethyl)-aspartamide)
  • alpha,beta-polyasparthydrazide
  • Suprofen
  • Glutaral