Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
9901408 | European Journal of Pharmaceutics and Biopharmaceutics | 2005 | 10 Pages |
Abstract
Baclofen was encapsulated in poly(lactide-co-glycolide) (PLGA) microspheres which were then dispersed in chitosan thermosensitive gels, Pluronic® PF-127 gels, carboxymethylcellulose solutions or Ringer lactate solution. The release rate was assessed in vitro using continuous flow cells and in vivo after intrathecal injection in goats: baclofen was quantified in cerebrospinal fluid (CSF) and plasma, and the associated pharmacological effect was evaluated. The results showed that the burst effect was reduced by at least a factor of 2 in vitro, after microsphere dispersion in viscous media. In vivo, PF-127 gel was found to be the best vehicle to reduce the burst effect by a factor of 10 in CSF, and by a factor of 2 in plasma. The toxic effect of baclofen due to the burst effect was reduced by the dispersion in PF127 gels. Therapeutic levels of baclofen in CSF were maintained during at least 1 month.
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Authors
Frederic Lagarce, Nathalie Faisant, Jean-Claude Desfontis, Laurent Marescaux, Freddy Gautier, Joel Richard, Philippe Menei, Jean-Pierre Benoit,