Synthesis and Evaluation of Transdermal Permeation, Pharmacological Activity of Bornyl NSAID Esters
Jiufeng Lin, Kefeng Ni, Yang Zhang, Dongzhi Wei and Yuhong Ren
Affiliation: State Key Laboratory of Bioreactor Engineering, New World Institute of Biotechnology, East China University of Science and Technology, Shanghai 200237, China.
Keywords: Anti-nociceptive, borneol, cyclooxygenase, esters, non-steroidal anti-inflammatory drugs, transdermal permeation.
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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