Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
2486159 | Journal of Pharmaceutical Sciences | 2011 | 7 Pages |
Abstract
Methylprednisolone (MP) released by poly(d,lâlactideâcoâglycolide) microspheres (PLGA MS) was monitored in plasma after intraâarticular (i.a.) administration into rat joint. A validated LCâESIâMS/MS method was used to quantify the plasmatic concentrations of MP. The calculated pharmacokinetic parameters were compared to those obtained after the i.a. administration of a commercially available suspension of MP acetate (MPA). Different pharmacokinetic profiles were observed in the two formulations, and a lower peak level (Cmax = 13.7 ± 4.3 ng·mLâ1) and AUC0-72 h (198 ± 45 ng·mLâ1·h) were observed for MPâPLGA MS than MPA (Cmax = 18.4 ± 2.7 ng·mLâ1) and AUC0-72 h (943 ± 249 ng·mLâ1·h). The administration of MPâPLGA MS resulted in a rapid increase in the MP concentration at 30 min, with a tmax at 0.8 ± 0.3 h. Instead, for the MPA suspension the tmax was 32.0 ± 13.9 h. These differences were indirectly confirmed by the evaluation of the extraâarticular effects, namely, carrageenanâinduced paw edema, since MPâPLGA MS showed a lower antiâinflammatory activity than MPA. © 2011 WileyâLiss, Inc. and the American Pharmacists Association J Pharm Sci 100:4580-4586, 2011
Keywords
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Pharmacology, Toxicology and Pharmaceutical Science
Drug Discovery
Authors
Alessia Panusa, Francesca Selmin, Giuseppe Rossoni, Marina Carini, Francesco Cilurzo, Giancarlo Aldini,