Phosphatidylcholine bilayers trigger the degradation of licofelone

• Main Authors: Catarina Pereira-Leite, Cláudia Nunes, Iolanda M. Cuccovia, Salette Reis
• Format: Article
• Language: English
• Published: ALIES - Associação Lusófona para o Desenvolvimento da Investigação e do Ensino das Ciências da Saúde 2019-06-01
• Series: Journal Biomedical and Biopharmaceutical Research (BBR)
• Subjects: anti-inflammatory drugs; dual cox-lox inhibitors; liposomes; uv-vis spectrophotometry
• Online Access: http://www.alies.pt/BBR%20Editions/Vol-16-2-2019/Art9.pdf

This is the first report, to the best of our knowledge, on the degradation of licofelone, a dual cyclooxygenaselipoxygenase inhibitor under development, in phosphatidylcholine bilayers. With the objective of characterizing licofelone-phosphatidylcholine interactions to understand its better gastric tolerability over conventional nonsteroidal anti-inflammatory drugs, our preliminary data showed that the lower the pH, the higher the rate and extent of licofelone degradation in the presence of phosphatidylcholine liposomes. The lipid concentration was another critical factor influencing the rate and extent of licofelone degradation, suggesting that phosphatidylcholine bilayers may act as a catalyst. These data highlight the need of considering lipids in drug development to better predict the drug pharmacokinetics prior to clinical evaluation.