A hydrogel based on a polyaspartamide: characterization and evaluation of in-vivo biocompatibility and drug release in the rat.
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.
Giammona
G
G
Dipartimento di Chimica e Tecnologie Farmaceutiche, Universitá di Palermo, Italy. gaegiamm@mbox.unipa.it
Pitarresi
G
G
Tomarchio
V
V
Cacciaguerra
S
S
Govoni
P
P
D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000009:adverse effects; D001682:Biological Availability; D004061:Diflunisal / Q000008:administration & dosage* / Q000009:adverse effects; D004337:Drug Carriers; D016503:Drug Delivery Systems; D005720:Gamma Rays; D020136:Hydrogel, Polyethylene Glycol Dimethacrylate; D006863:Hydrogen-Ion Concentration; D008297:Male; D008863:Microspheres; D011092:Polyethylene Glycols / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013276:Stomach Ulcer / Q000139:chemically induced / Q000473:pathology / Q000517:prevention & control
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D020136:Hydrogel, Polyethylene Glycol Dimethacrylate; D011092:Polyethylene Glycols; D004061:Diflunisal