Diclofenac Prodrugs for Intra-articular Depot Injectables: In Vitro Hydrolysis and Species Variation

Storgaard, Ida Hagen; Kristensen, Jesper L.; Larsen, Claus; Mertz, Nina; Østergaard, Jesper; Larsen, Susan Weng

doi:10.1016/j.xphs.2020.01.003

Cited by 3 publications

(3 citation statements)

References 37 publications

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“…This study of another diclofenac depo-injectable reported increased diclofenac half-life in horse synovial fluid (Storgaard et al, 2020).…”

Section: Discussionmentioning

confidence: 72%

“…This was successfully achieved, as shown by a substantial increase in diclofenac half‐life in synovial fluid and by rather consistent total and free diclofenac concentrations in synovial fluid over time (Figures 2 and 3). A recent in vitro study of another diclofenac depo‐injectable reported increased diclofenac half‐life in horse synovial fluid (Storgaard et al, 2020). However, to the best of our knowledge, no pharmacodynamic data (potency and efficacy values) have been published previously for diclofenac in vivo in horses.…”

Section: Discussionmentioning

confidence: 99%

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In vivo joint synovial fluid disposition of a novel sustained‐release formulation of diclofenac and hyaluronic acid in horses

Rhodin

Andersen

Forsström

et al. 2021

Vet Pharm & Therapeutics

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Osteoarthritis (OA) is the most common type of degenerative joint disease in horses (Goodrich & Nixon, 2006) and humans (Moskowitz, 2009). The disease is a major source of pain, disability and socioeconomic cost worldwide (Woolf & Pfleger, 2003), and results in severe welfare issues and economic losses for humans and for horse-related industries.Osteoarthritis is a complex disease that involves all parts of the joint. It may be caused by a number of different factors, ranging from chronic low-grade micro insults to acute trauma and infection. The involvement of inflammation produced by synovium and chondrocytes is central to the pathogenesis, with inflammatory cytokines, metalloproteases and other inflammatory mediators being present in synovial fluid of patients with OA (2006). The resulting joint pain manifests as lameness (Schlueter & Orth, 2004) and the joint capsule inflammation causes swelling and fibrosis, resulting in additional pain and decreased range of motion of the affected joint. No curative treatments exist for this disease, but early symptomatic treatment can reduce pain and the cartilage-damaging effects of the inflammatory products, and decrease the progression of cartilage destruction and fibrosis of the joint capsule (Goldring & Otero, 2011). In horses, a common treatment regime consists of systemic administration of non-steroidal antiinflammatory drugs (NSAIDs; Goodrich & Nixon, 2006).

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“…This study of another diclofenac depo-injectable reported increased diclofenac half-life in horse synovial fluid (Storgaard et al, 2020).…”

Section: Discussionmentioning

confidence: 72%

Section: Discussionmentioning

confidence: 99%

In vivo joint synovial fluid disposition of a novel sustained‐release formulation of diclofenac and hyaluronic acid in horses

Rhodin

Andersen

Forsström

et al. 2021

Vet Pharm & Therapeutics

View full text Add to dashboard Cite

show abstract

“…S17 ), showing how our conjugates can also become a substrate for active enzymatic cleavage. Though the synovial fluid is known to also contain esterases [ 75 ], the concentrations are generally rather low so we expect the physiological release kinetics to be mainly driven by passive carbonate-catalyzed hydrolysis.…”

Section: Resultsmentioning

confidence: 99%

Zwitterionic polymer-dexamethasone conjugates penetrate and protect cartilage from inflammation

Weber,

Asadikorayem,

Surman

et al. 2024

Materials Today Bio

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In situ monitoring of the formation of lipidic non-lamellar liquid crystalline depot formulations in synovial fluid

Yaghmur

Rappolt

Jonassen

et al. 2021

Journal of Colloid and Interface Science

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Diclofenac Prodrugs for Intra-articular Depot Injectables: In Vitro Hydrolysis and Species Variation

Cited by 3 publications

References 37 publications

In vivo joint synovial fluid disposition of a novel sustained‐release formulation of diclofenac and hyaluronic acid in horses

In vivo joint synovial fluid disposition of a novel sustained‐release formulation of diclofenac and hyaluronic acid in horses

Zwitterionic polymer-dexamethasone conjugates penetrate and protect cartilage from inflammation

In situ monitoring of the formation of lipidic non-lamellar liquid crystalline depot formulations in synovial fluid

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