Abstract
The bornyl ester derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) including naproxen, ketoprofen and flufenamic acid, were synthesized and their transdermal permeation efficiency and pharmacological activity were determined. The bornyl NSAID esters exhibited more than 10-fold increase of permeation efficiency across mice skin than parent NSAIDs. The preliminary biological and pharmacological evaluations suggested that the bornyl NSAID esters retain most of their inhibition activity toward cyclooxygenase (COX) enzymes and show significant analgesic effect against acetic acid-induced writhing in mice.
Keywords: Anti-nociceptive, borneol, cyclooxygenase, esters, non-steroidal anti-inflammatory drugs, transdermal permeation.
Letters in Drug Design & Discovery
Title:Synthesis and Evaluation of Transdermal Permeation, Pharmacological Activity of Bornyl NSAID Esters
Volume: 12 Issue: 1
Author(s): Jiufeng Lin, Kefeng Ni, Yang Zhang, Dongzhi Wei and Yuhong Ren
Affiliation:
Keywords: Anti-nociceptive, borneol, cyclooxygenase, esters, non-steroidal anti-inflammatory drugs, transdermal permeation.
Abstract: The bornyl ester derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) including naproxen, ketoprofen and flufenamic acid, were synthesized and their transdermal permeation efficiency and pharmacological activity were determined. The bornyl NSAID esters exhibited more than 10-fold increase of permeation efficiency across mice skin than parent NSAIDs. The preliminary biological and pharmacological evaluations suggested that the bornyl NSAID esters retain most of their inhibition activity toward cyclooxygenase (COX) enzymes and show significant analgesic effect against acetic acid-induced writhing in mice.
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Cite this article as:
Lin Jiufeng, Ni Kefeng, Zhang Yang, Wei Dongzhi and Ren Yuhong, Synthesis and Evaluation of Transdermal Permeation, Pharmacological Activity of Bornyl NSAID Esters, Letters in Drug Design & Discovery 2015; 12 (1) . https://dx.doi.org/10.2174/1570180811666140627004820
DOI https://dx.doi.org/10.2174/1570180811666140627004820 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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