Methylprednisolone (MP) released by poly(d,l-lactide-co-glycolide) microspheres (PLGA MS) was monitored in plasma after intra-articular (i.a.) administration into rat joint. A validated LC-ESI-MS/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 (C(max) = 13.7 ± 4.3 ng · mL(-1)) and AUC(0-72 h) (198 ± 45 ng · mL(-1) · h) were observed for MP-PLGA MS than MPA (C(max) = 18.4 ± 2.7 ng · mL(-1)) and AUC(0-72 h) (943 ± 249 ng · mL(-1) · h). The administration of MP-PLGA MS resulted in a rapid increase in the MP concentration at 30 min, with a t(max) at 0.8 ± 0.3 h. Instead, for the MPA suspension the t(max) was 32.0 ± 13.9 h. These differences were indirectly confirmed by the evaluation of the extra-articular effects, namely, carrageenan-induced paw edema, since MP-PLGA MS showed a lower anti-inflammatory activity than MPA.
Methylprednisolone-loaded PLGA microspheres: A new formulation for sustained release via intra-articular administration. A comparison study with methylprednisolone acetate in rats / A. Panusa, F. Selmin, G.B. Rossoni, M. Carini, F. Cilurzo, G. Aldini. - In: JOURNAL OF PHARMACEUTICAL SCIENCES. - ISSN 0022-3549. - 100:11(2011 Nov), pp. 4580-4586.
|Titolo:||Methylprednisolone-loaded PLGA microspheres: A new formulation for sustained release via intra-articular administration. A comparison study with methylprednisolone acetate in rats|
PANUSA, ALESSIA (Primo)
SELMIN, FRANCESCA (Secondo)
CILURZO, FRANCESCO (Penultimo)
ALDINI, GIANCARLO (Ultimo)
|Parole Chiave:||Analysis; Mass spectrometry; Methylprednisolone; Methylprednisolone acetate; Microspheres; Pharmacokinetics; Poly(lactic/glycolic) acid (PLGA)|
|Settore Scientifico Disciplinare:||Settore CHIM/08 - Chimica Farmaceutica|
Settore CHIM/09 - Farmaceutico Tecnologico Applicativo
Settore BIO/14 - Farmacologia
|Data di pubblicazione:||nov-2011|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1002/jps.22722|
|Appare nelle tipologie:||01 - Articolo su periodico|