Penetration and efficacy of transdermal NSAIDs in a model of acute joint inflammation

Prescription and OTC non-steroidal anti-inflammatory drugs (NSAIDs) are ubiquitous treatments for pain and inflammation; however, oral administration of these drugs may produce gastrointestinal (GI) side effects. Transdermal (TD) administration of NSAIDs circumvents these adverse events by avoiding...

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Bibliographic Details
Published in:Journal of pain research 2018-01, Vol.11, p.2809-2819
Main Authors: Baranowski, David Charles, Buchanan, Beth, Dwyer, Heather C, Gabriele, Joseph P, Kelly, Stephanie, Araujo, Joseph A
Format: Article
Language:English
Subjects:
Analgesia
Analgesics
Analysis
Anti-inflammatory agents
canine model
Care and treatment
celecoxib
Chromatography
Complications and side effects
Dogs
Gastrointestinal system
Ibuprofen
Inflammation
Laboratories
Liquid chromatography
Nonprescription drugs
Nonsteroidal anti-inflammatory agents
Nonsteroidal anti-inflammatory drugs
Original Research
Osteoarthritis
Pain
Pain management
R&D
Research & development
Rheumatism
Rheumatoid arthritis
Sodium
Spectroscopy
Steroidal anti-inflammatory agents
Topical analgesics
Transdermal drug delivery systems
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Summary:Prescription and OTC non-steroidal anti-inflammatory drugs (NSAIDs) are ubiquitous treatments for pain and inflammation; however, oral administration of these drugs may produce gastrointestinal (GI) side effects. Transdermal (TD) administration of NSAIDs circumvents these adverse events by avoiding the GI tract and, presumably, achieves regional drug levels of therapeutic effect and thereby, fewer off-target complications. A drug quantification method was developed for ibuprofen and celecoxib in canine plasma and synovial fluid using liquid chromatography and mass spectrometry. This method was employed to evaluate the penetrance of ibuprofen and celecoxib topical formulations in dogs. Effectiveness of these topical NSAID formulations was compared to the equivalent oral drug concentration in a canine sodium-urate model of acute joint inflammation. In this model, pain was quantified using a modified Canine Brief Pain Inventory questionnaire and regional inflammation using joint caliper measurements; the significance of intervention was evaluated using linear mixed models for repeated measures along with Bonferroni corrections. After seven days of chronic topical administration, Delivra™ (DEL) formulations of ibuprofen and celecoxib generated serum levels of 2.9µg/mL and 220ng/mL and synovial fluid levels of 1.8 µg/mL and 203 ng/mL (respectively). In the canine model of acute inflammation, the overall treatment effects as well as the treatment by time interactions were strongly significant (
ISSN:1178-7090
1178-7090
DOI:10.2147/JPR.S177967