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In vitro evaluation of S-(+)-ibuprofen as drug candidate for intra-articular drug delivery system |
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| Authors: | Laurent Bédouet Florentina Pascale Michel Bonneau Alexandre Laurent |
| Affiliation: | 1. Occlugel SAS, Jouy-en-Josas, France,;2. AP-HP, INRA, Center for Research of Interventional Imaging (CR2i), Jouy-en-Josas, France, and;3. Occlugel SAS, Jouy-en-Josas, France,;4. AP-HP, INRA, Center for Research of Interventional Imaging (CR2i), Jouy-en-Josas, France, and;5. Department of Interventional Neuroradiology, AP-HP, Lariboisière Hospital, Paris, France |
| Abstract: | Intra-articular drug delivery systems (DDSs) are envisaged as interesting alternative to locally release non-steroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen to reduce pain in patients with osteoarthritis. The present study examines the efficacy of S-(+)-ibuprofen on cartilage degradation as drug candidate for DDS loading. Humeral cartilage and joint capsule explants were collected from healthy sheep shoulder joints and they were cultured in mono- or in co-culture for 13?days with LPS in combination with S-(+)-ibuprofen at 50?µM and 1?mM. S-(+)-ibuprofen (50?µM) blocked prostaglandins production in LPS-activated explants but did not reduce cartilage degradation. By contrast, 1?mM S-(+)-ibuprofen treatment of cartilage explants reduced nitric oxide synthesis by 51% (p?=?0.0072), proteoglycans degradation by 35% (p?=?0.0114) and expression of serum amyloid protein – the main protein induced upon LPS challenge – by 44% (p? |
| Keywords: | Cartilage co-culture drug delivery systems osteoarthritis S-(+)-ibuprofen |
