A hydrogel based on a polyaspartamide: characterization and evaluation of in-vivo biocompatibility and drug release in the rat

J Pharm Pharmacol. 1997 Nov;49(11):1051-6. doi: 10.1111/j.2042-7158.1997.tb06040.x.

Abstract

This paper deals with the characterization of a new microparticulate hydrogel obtained by gamma irradiation of alpha, beta-poly[N-(2-hydroxyethyl)-DL-aspartamide] (PHEA). When enzymatic digestion of PHEA hydrogel was evaluated using various concentrations of pepsin and alpha-chymotrypsin no degradation occurred within 24 h. In-vivo studies showed that this new material is biocompatible after oral administration to rats. PHEA hydrogel was also studied as a system for delivery of diflunisal, an anti-inflammatory drug. In-vitro release studies in simulated gastrointestinal juice (pH 1 or 6.8) showed that most of the drug was released at pH 6.8. In-vivo studies indicated that diflunisal-loaded PHEA microparticles significantly improved the gastric tolerance and oral bioavailability of the drug in comparison with free diflunisal. These results suggest the potential application of PHEA hydrogel as a new delivery system for the oral administration of anti-inflammatory drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage*
  • Anti-Inflammatory Agents, Non-Steroidal / adverse effects
  • Biological Availability
  • Diflunisal / administration & dosage*
  • Diflunisal / adverse effects
  • Drug Carriers
  • Drug Delivery Systems
  • Gamma Rays
  • Hydrogel, Polyethylene Glycol Dimethacrylate
  • Hydrogen-Ion Concentration
  • Male
  • Microspheres
  • Polyethylene Glycols / chemistry
  • Polyethylene Glycols / pharmacokinetics*
  • Rats
  • Rats, Sprague-Dawley
  • Stomach Ulcer / chemically induced
  • Stomach Ulcer / pathology
  • Stomach Ulcer / prevention & control

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Drug Carriers
  • Hydrogel, Polyethylene Glycol Dimethacrylate
  • Polyethylene Glycols
  • Diflunisal