Synthesis and Evaluation of Transdermal Permeation, Pharmacological Activity of Bornyl NSAID Esters
Jiufeng Lin, Kefeng Ni, Yang Zhang, Dongzhi Wei and Yuhong Ren
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 exhibit more than 10-fold increase of permeation efficiency across mice skin than parent NSAIDs. The preliminary biological and pharmacological evaluations suggest that the bornyl NSAID esters retain most of its inhibition activity toward cyclooxygenase (COX) enzymes and show significant analgesic effect against acetic acid-induced writhing in mice.
Non-steroidal anti-inflammatory drugs, Borneol, Esters, Transdermal permeation, Cyclooxygenase, Antinociceptive
State Key Laboratory of Bioreactor Engineering New World Institute of Biotechnology East China University of Science and Technology Shanghai 200237 China.