PMID- 24168233
OWN - NLM
STAT- MEDLINE
DCOM- 20150824
LR  - 20141217
IS  - 1520-5762 (Electronic)
IS  - 0363-9045 (Linking)
VI  - 41
IP  - 1
DP  - 2015 Jan
TI  - In vitro evaluation of S-(+)-ibuprofen as drug candidate for intra-articular drug 
      delivery system.
PG  - 85-94
LID - 10.3109/03639045.2013.850704 [doi]
AB  - 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 microM 
      and 1 mM. S-(+)-ibuprofen (50 microM) 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 < 0.0001). On contrary, in presence of synovial membrane, the 
      protective effects of S-(+)-ibuprofen on cartilage damages were significantly 
      diminished. At 1mM, S-(+)-ibuprofen reduced the cell lysis during culture of 
      cartilage and joint capsule either in mono- or in co-culture. This study 
      performed on sheep explants shows that 1 mM S-(+)-ibuprofen inhibited cartilage 
      degradation via a mechanism independent of cyclooxygenase inhibition. Reduction 
      of prostaglandins synthesis at 50 microM in all treatment groups and reduction of 
      cartilage degradation observed at 1 mM suggest that S-(+)-ibuprofen could be 
      considered as a promising drug candidate for the loading of intra-articular DDS.
FAU - Bedouet, Laurent
AU  - Bedouet L
AD  - Occlugel SAS, Jouy-en-Josas , France .
FAU - Pascale, Florentina
AU  - Pascale F
FAU - Bonneau, Michel
AU  - Bonneau M
FAU - Laurent, Alexandre
AU  - Laurent A
LA  - eng
PT  - Journal Article
DEP - 20131030
PL  - England
TA  - Drug Dev Ind Pharm
JT  - Drug development and industrial pharmacy
JID - 7802620
RN  - 0 (Anti-Inflammatory Agents, Non-Steroidal)
RN  - WK2XYI10QM (Ibuprofen)
SB  - IM
MH  - Animals
MH  - Anti-Inflammatory Agents, Non-Steroidal/*administration & 
      dosage/*chemistry/metabolism
MH  - Coculture Techniques/methods
MH  - Drug Delivery Systems/*methods
MH  - Drug Evaluation, Preclinical/methods
MH  - Ibuprofen/*administration & dosage/*chemistry/metabolism
MH  - Injections, Intra-Articular
MH  - Sheep
MH  - Synovial Membrane/drug effects/metabolism
OTO - NOTNLM
OT  - Cartilage
OT  - S-(+)-ibuprofen
OT  - co-culture
OT  - drug delivery systems
OT  - osteoarthritis
EDAT- 2013/10/31 06:00
MHDA- 2015/08/25 06:00
CRDT- 2013/10/31 06:00
PHST- 2013/10/31 06:00 [entrez]
PHST- 2013/10/31 06:00 [pubmed]
PHST- 2015/08/25 06:00 [medline]
AID - 10.3109/03639045.2013.850704 [doi]
PST - ppublish
SO  - Drug Dev Ind Pharm. 2015 Jan;41(1):85-94. doi: 10.3109/03639045.2013.850704. Epub 
      2013 Oct 30.