title: Celecoxib-loaded PLGA/cyclodextrin microspheres: characterization and evaluation of anti-inflammatory activity on human chondrocyte cultures.
abstract: PLGA microspheres were prepared as a sustained release system for the intra-articular administration of celecoxib (CCB). The microspheres were prepared in the presence of different concentrations of dimethyl-β-cyclodextrin (DM-β-Cyd), by the simple oil-in-water emulsion/evaporation solvent method. The microspheres were evaluated as to surface morphology, size and technological properties (such as encapsulation efficiency, drug loading capacity and drug release). Ex vivo studies on cultures of human chondrocytes were performed in order to evaluate the influence of the polymeric carriers on the pharmacological activity of CCB. All systems ranged from about 1 to 5 μm in size and had a high encapsulation efficiency percentage ranging from about 80% to 90% (w/w), except for CCB-loaded-PLGA microspheres containing the highest amount of DM-β-Cyd, in which a dramatic drop in the encapsulation efficiency was observed (about 54%, w/w). FIB images evidenced the fact that the microspheres had a porous structure in the presence of the highest amount of DM-β-Cyd. The macrocycle modulated the release profiles of CCB from the microspheres, producing in some cases a zero-order kinetic release. Ex vivo biological studies demonstrated that DM-β-Cyd improved the drug's anti-inflammatory activity. Thus, CCB-loaded PLGA/cyclodextrin microspheres may have a potential therapeutic application in the treatment of osteo- and rheumatoid arthritis.
authors.affiliation: Dipartimento di Scienze del Farmaco e dei Prodotti per la Salute, Università degli Studi di Messina, V. le Annunziata, I-98168 Messina, Italy.
authors.forename: Carmela
authors.initials: C
authors.lastname: Cannavà
authors.affiliation: Dipartimento di Scienze del Farmaco e dei Prodotti per la Salute, Università degli Studi di Messina, V. le Annunziata, I-98168 Messina, Italy.
authors.forename: Silvana
authors.initials: S
authors.lastname: Tommasini
authors.affiliation: Dipartimento di Scienze del Farmaco e dei Prodotti per la Salute, Università degli Studi di Messina, V. le Annunziata, I-98168 Messina, Italy.
authors.forename: Rosanna
authors.initials: R
authors.lastname: Stancanelli
authors.affiliation: Dipartimento di Scienze Biomediche (Sezione di Fisiologia), Università degli Studi di Catania, Città Universitaria, V. le A. Doria, 6 - I-95125 Catania, Italy.
authors.forename: Venera
authors.initials: V
authors.lastname: Cardile
authors.affiliation: Dipartimento di Scienze della Salute, Università Magna Graecia di Catanzaro, Viale Europa 88100, Loc. Germaneto Catanzaro, Italy.
authors.forename: Felisa
authors.initials: F
authors.lastname: Cilurzo
authors.affiliation: Dipartimento di Scienze del Farmaco, Università degli Studi di Catania, Città Universitaria, V. le A. Doria, 6 - I-95125 Catania, Italy.
authors.forename: Ignazio
authors.initials: I
authors.lastname: Giannone
authors.affiliation: Dipartimento di Scienze del Farmaco, Università degli Studi di Catania, Città Universitaria, V. le A. Doria, 6 - I-95125 Catania, Italy.
authors.forename: Giovanni
authors.initials: G
authors.lastname: Puglisi
authors.affiliation: Dipartimento di Scienze del Farmaco e dei Prodotti per la Salute, Università degli Studi di Messina, V. le Annunziata, I-98168 Messina, Italy. Electronic address: caventura@unime.it.
authors.forename: Cinzia Anna
authors.initials: CA
authors.lastname: Ventura
mesh_terms: D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D002152:Calorimetry, Differential Scanning; D000068579:Celecoxib; D002478:Cells, Cultured; D019902:Chondrocytes / Q000166:cytology* / Q000187:drug effects; D002942:Circular Dichroism; D003505:Cyclodextrins / Q000737:chemistry*; D004008:Diclofenac / Q000494:pharmacology; D004058:Diffusion; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D008863:Microspheres; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011720:Pyrazoles / Q000494:pharmacology*; D013449:Sulfonamides / Q000494:pharmacology*
chemical_list: D000893:Anti-Inflammatory Agents; D003505:Cyclodextrins; D011720:Pyrazoles; D013449:Sulfonamides; D004008:Diclofenac; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D000068579:Celecoxib
keywords: Celecoxib; Chondrocyte cultures; Dimethyl-β-cyclodextrin; PLGA microspheres; Release kinetics