2012
DOI: 10.2460/ajvr.73.10.1530
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Concentration-dependent effects of tiludronate on equine articular cartilage explants incubated with and without interleukin-1β

Abstract: Tiludronate had biphasic concentration-dependent effects on cartilage explants that were independent of PGE(2) secretion or MMP gene expression. Low tiludronate concentrations had some chondroprotective effects, whereas high tiludronate concentrations were detrimental to equine articular cartilage. Administration of tiludronate intra-articularly to horses may be detrimental, dependent on the dose used. In vivo studies are needed before intra-articular tiludronate administration to horses can be recommended.

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Cited by 14 publications
(41 citation statements)
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“…The target tissue for tiludronate has traditionally been bone (EMEA, 2001), but tiludronate also exerts direct effects on cartilage and chondrocytes (Duesterdieck-Zellmer, Driscoll & Ott, 2012; Emonds-Alt, Breliere & Roncucci, 1985), especially after extra-label local administration via regional limb perfusion or intraarticular injection, since these routes of administration potentially result in high synovial fluid concentrations. In-vitro data suggests that synovial fluid tiludronate concentrations of 19,000 ng/mL and above promote chondrocyte apoptosis and release of sGAGs from articular cartilage matrix, whereas concentrations of 1,900 ng/mL and below may ameliorate sGAG release and chondrocyte apoptosis in equine joints (Duesterdieck-Zellmer, Driscoll & Ott, 2012).…”
Section: Discussionmentioning
confidence: 99%
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“…The target tissue for tiludronate has traditionally been bone (EMEA, 2001), but tiludronate also exerts direct effects on cartilage and chondrocytes (Duesterdieck-Zellmer, Driscoll & Ott, 2012; Emonds-Alt, Breliere & Roncucci, 1985), especially after extra-label local administration via regional limb perfusion or intraarticular injection, since these routes of administration potentially result in high synovial fluid concentrations. In-vitro data suggests that synovial fluid tiludronate concentrations of 19,000 ng/mL and above promote chondrocyte apoptosis and release of sGAGs from articular cartilage matrix, whereas concentrations of 1,900 ng/mL and below may ameliorate sGAG release and chondrocyte apoptosis in equine joints (Duesterdieck-Zellmer, Driscoll & Ott, 2012).…”
Section: Discussionmentioning
confidence: 99%
“…In-vitro data suggests that synovial fluid tiludronate concentrations of 19,000 ng/mL and above promote chondrocyte apoptosis and release of sGAGs from articular cartilage matrix, whereas concentrations of 1,900 ng/mL and below may ameliorate sGAG release and chondrocyte apoptosis in equine joints (Duesterdieck-Zellmer, Driscoll & Ott, 2012). Subsequently, the dose for the LDT group was chosen to produce synovial fluid tiludronate concentrations approximating 1,900 ng/mL.…”
Section: Discussionmentioning
confidence: 99%
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