Skin Permeability and Local Tissue Concentrations of Nonsteroidal Antiinflammatory Drugs After Topical Application

Singh, P and Roberts, MS (1994) Skin Permeability and Local Tissue Concentrations of Nonsteroidal Antiinflammatory Drugs After Topical Application. Journal of Pharmacology and Experimental Therapeutics, 268 1: 144-151.

Author Singh, P
Roberts, MS
Title Skin Permeability and Local Tissue Concentrations of Nonsteroidal Antiinflammatory Drugs After Topical Application
Journal name Journal of Pharmacology and Experimental Therapeutics   Check publisher's open access policy
ISSN 0022-3565
Publication date 1994-01-01
Year available 1994
Sub-type Article (original research)
Open Access Status Not yet assessed
Volume 268
Issue 1
Start page 144
End page 151
Total pages 8
Place of publication BALTIMORE
Publisher WILLIAMS & WILKINS
Language eng
Abstract Nonsteroidal anti-inflammatory drugs (NSAIDs) are being administered increasingly by transdermal drug delivery for the treatment of local muscle inflammation. The human epidermal permeabilities of different NSAIDs (salicylic acid, diethylamine salicylate, indomethacin, naproxen, diclofenac and piroxicam) from aqueous solutions is dependent on the drug's lipophilicity. A parabolic relationship was observed when the logarithms of NSAID permeability coefficients were plotted against the logarithms of NSAID octanol-water partition coefficients (log P), the optimum log P being around 3. The local tissue concentrations of these drugs after dermal application in aqueous solutions were then determined in a rat model. The extent of local, as distinct from systemic delivery, for each NSAID was assessed by comparing the tissue concentrations obtained below a treated site to those in contralateral tissues. Local direct penetration was evident for all NSAIDs up to a depth of about 3 to 4 mm below the applied site, with distribution to deeper tissues being mainly through the systemic blood supply. A comparison of the predicted tissue concentrations of each NSAID after its application to human epidermis was then made by a convolution of the epidermal and underlying tissue concentration-time profiles. The estimated tissue concentrations after epidermal application of NSAIDs could be related to their maximal fluxes across epidermis from an applied vehicle.
Keyword Absorption
Penetration
Salicylate
Muscle
Model
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Unknown

Document type: Journal Article
Sub-type: Article (original research)
Collection: ResearcherID Downloads - Archived
 
Versions
Version Filter Type
Citation counts: TR Web of Science Citation Count  Cited 173 times in Thomson Reuters Web of Science Article | Citations
Google Scholar Search Google Scholar
Created: Wed, 02 Nov 2011, 23:09:19 EST by System User