Self promotion of deep tissue penetration and distribution of methylsalicylate after topical application

Cross, SE, Megwa, SA, Benson, HAE and Roberts, MS (1999) Self promotion of deep tissue penetration and distribution of methylsalicylate after topical application. Pharmaceutical Research, 16 3: 427-433. doi:10.1023/A:1018834021066


Author Cross, SE
Megwa, SA
Benson, HAE
Roberts, MS
Title Self promotion of deep tissue penetration and distribution of methylsalicylate after topical application
Journal name Pharmaceutical Research   Check publisher's open access policy
ISSN 0724-8741
Publication date 1999-01-01
Year available 1999
Sub-type Article (original research)
DOI 10.1023/A:1018834021066
Open Access Status Not yet assessed
Volume 16
Issue 3
Start page 427
End page 433
Total pages 7
Place of publication New York
Publisher Plenum
Language eng
Subject C1
730117 Skin and related disorders
320501 Pharmaceutical Sciences and Pharmacy
Abstract Purpose. To determine how changes in cutaneous blood flow induced in-vivo by methylsalicylate (MeSA), compared to non-rubefacient triethanolamine salicylate (TSA), affected topical salicylate absorption and distribution, and to assess formulation therapeutic potential by comparing tissue concentrations to published antiinflammatory concentrations. Methods. Flux of salicylate from MeSA and TSA formulations applied to Full-thickness rat skin was determined using in vitro diffusion cells. Anaesthetised rats were then used to quantify salicylate concentrations in plasma and tissues underlying the application site for the two formulations over a 6h period. In vitro and in vivo absorption profiles were then compared and the effect of MeSA on cutaneous blood flow assessed. Results. In vitro flux of salicylate from the MeSA formulation was 40% higher, though after correcting for differences in formulation concentrations the ratio of permeability coefficients was reversed. Contrary to the in vitro predictions, in vivo tissue and plasma concentrations of salicylate in rats rose rapidly in the first 1 hr and were more than the predicted 1.4-fold higher for MeSA. This effect was mirrored by the increase in blood flow induced by MeSA in human cutaneous vessels and that reported in the literature. Potential therapeutic levels were not seen below superficial muscle layers. Conclusions. Direct tissue penetration of salicylate occurs below application sites from both MeSA and TSA formulations. Tissue concentrations of MeSA were higher than predicted due to its rapid distribution in the blood.
Keyword Chemistry, Multidisciplinary
Pharmacology & Pharmacy
Rats
Percutaneous
Salicylates
Metabolism
Methyl Salicylate
Warfarin Anticoagulation
Percutaneous-absorption
Acid
Pharmacokinetics
Mechanisms
Ointment
Delivery
Drugs
Skin
Q-Index Code C1
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collection: School of Medicine Publications
 
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Created: Wed, 11 Jun 2008, 00:31:40 EST