NSAIDs Interactions with Membranes: A Biophysical Approach

• DOI: 10.1021/la201600y
• Publication Date: 2011-07-26T19:47:49Z
• Authors: Cláudia Nunes; Gerald Brezesinski; Catarina Pereira-...; José L. F. C. Lima; Salette Reis; Marlene Lúcio
• Keywords: Microviscosity; Membrane biophysics; POPC; Meloxicam

This work focuses on the interaction of four representative NSAIDs (nimesulide, indomethacin, meloxicam, and piroxicam) with different membrane models (liposomes, monolayers, supported lipid bilayers), at pH values, that mimic conditions normal (pH 7.4) inflamed cells 5.0). All are composed 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) which is a phospholipid most cellular membranes. Several biophysical techniques were employed: Fluorescence steady-state anisotropy to study effects in microviscosity thus assess main phase transition DPPC, surface pressure–area isotherms evaluate adsorption penetration into membrane, IRRAS acquire structural information DPPC monolayers upon drugs, AFM changes topography bilayers caused by NSAIDs. The show pronounced interactions membranes both physiological inflammatory conditions. Liposomes, experiments allow conclusion medium an essential parameter when evaluating drug–membrane interactions, because it structure ionization state NSAIDs, thereby influencing between these drugs applied provided detailed about aspects offering valuable understand effect their target membrane-associated enzymes side gastrointestinal level.