Synthesis and Evaluation of Transdermal Permeation, Pharmacological Activity of Bornyl NSAID Esters

Author(s): Jiufeng Lin, Kefeng Ni, Yang Zhang, Dongzhi Wei, Yuhong Ren.

Journal Name: Letters in Drug Design & Discovery

Volume 12 , Issue 1 , 2015

Graphical 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.

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Article Details

Year: 2015
Page: [72 - 77]
Pages: 6
DOI: 10.2174/1570180811666140627004820

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PDF: 33