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  • Intra-articular (IA) ropivacaine microparticle suspensions reduce pain, inflammation, cytokine, and substance p levels significantly more than oral or IA celecoxib in a rat model of arthritis.

Intra-articular (IA) ropivacaine microparticle suspensions reduce pain, inflammation, cytokine, and substance p levels significantly more than oral or IA celecoxib in a rat model of arthritis.

Inflammation (2014-09-06)
Barrett Rabinow, Jane Werling, Alison Bendele, Jerome Gass, Roy Bogseth, Kelly Balla, Paul Valaitis, Audrey Hutchcraft, Sabine Graham
RESUMEN

Current therapeutic treatment options for osteoarthritis entail significant safety concerns. A novel ropivacaine crystalline microsuspension for bolus intra-articular (IA) delivery was thus developed and studied in a peptidoglycan polysaccharide (PGPS)-induced ankle swelling rat model. Compared with celecoxib controls, both oral and IA, ropivacaine IA treatment resulted in a significant reduction of pain upon successive PGPS reactivation, as demonstrated in two different pain models, gait analysis and incapacitance testing. The reduction in pain was attended by a significant reduction in histological inflammation, which in turn was accompanied by significant reductions in the cytokines IL-18 and IL-1β. This may have been due to inhibition of substance P, which was also significantly reduced. Pharmacokinetic analysis indicated that the analgesic effects outlasted measurable ropivacaine levels in either blood or tissue. The results are discussed in the context of pharmacologic mechanisms both of local anesthetics as well as inflammatory arthritis.

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Supelco
Phosphate Standard for IC, TraceCERT®, 1000 mg/L phosphate in water
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Sodium phosphate monobasic-16O4, 99.9 atom % 16O
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Sodium phosphate dibasic solution, BioUltra, 0.5 M in H2O
Celecoxib, European Pharmacopoeia (EP) Reference Standard
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Sodium phosphate monobasic, ReagentPlus®, ≥99.0%
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Sodium phosphate dibasic, BioReagent, suitable for cell culture, suitable for insect cell culture, ≥99.0%
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Sodium phosphate monobasic, BioReagent, for molecular biology, anhydrous, ≥98%
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Sodium phosphate dibasic, for molecular biology, ≥98.5% (titration)
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1,2-Dimyristoyl-sn-glycero-3-phospho-rac-(1-glycerol) sodium salt, ≥99%
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Sodium phosphate monobasic, BioXtra, ≥99.0%
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Sodium phosphate dibasic, 99.95% trace metals basis
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Sodium phosphate monobasic, 99.998% trace metals basis
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Sodium phosphate monobasic, purum p.a., anhydrous, ≥99.0% (T)
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Sodium phosphate monobasic, anhydrous, free-flowing, Redi-Dri, ≥99.0%
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Sodium phosphate dibasic, ACS reagent, ≥99.0%
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