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    Meloxicam and Meloxicam-b-Cyclodextrin Complex in Model Membranes: Effects on the Properties and Enzymatic Lipolysis of Phospholipid Monolayers in Relation to Anti-inflammatory Activity

    Year: 2009

    Journal: Langmuir 25 (2009) 1417-1426, 20111221

    Authors: Katarzyna Wieclaw, Beata Korchowiec, Yohann Corvis, Jacek Korchowiec, Hassan Guermouche and Ewa Rogalska

    Organizations: Department of Physical Chemistry and Electrochemistry, Faculty of Chemistry, Jagiellonian University, ul. R. Ingardena 3, 30-060 Krakow, Poland, Structure et Réactivité des Systémes Moléculaires Complexes, BP 239, CNRS/Nancy Université, 54506 Vandoeuvre-lés-Nancy cedex, France, Department of Theoretical Chemistry, Faculty of Chemistry, Jagiellonian University, ul. R. Ingardena 3, 30-060 Krakow, Poland, and Faculté de Chimie, USTHB, B.P. No. 32, El-Alia, Bab-Ezzouar, Alger, Algeria

    Meloxicam, a nonsteroidal anti-inflammatory drug (NSAID), is known as a selective cyclooxygenase-2 inhibitor. Cyclooxygenase-2 is a membrane protein, functionally coupled to an interfacial enzyme, phospholipase A2. Consequently,it may be supposed that the interactions of NSAIDs with lipid membranes play a role in the anti-inflammatory process. In order to investigate the mechanism of this process, Langmuir films formed with 1,2-dipalmitoyl-sn-glycero-3-phosphocholine, 1,2-dilauroyl-sn-glycero-3-phosphocholine, 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine, or 1,2-myristoyl-sn-glycero-3-phosphoethanolamine were exposed to meloxicam and its -cyclodextrin inclusion complex.The monolayers were studied by measuring surface pressure, electric surface potential, Brewster angle micrographs,polarization-modulation infrared reflection-absorption spectra, and phospholipase A2 activity; the inclusion complex was studied using molecular modeling. The results obtained show that the monolayers formed in the presence of meloxicam and its complex are expanded and more liquid-like compared to pure lipids. Both compounds modify hydration of the lipid polar heads, orientation of the molecules, morphology of the domains, and the rate of lipolysis catalyzed by phospholipase A2. The latter effect may be involved in the anti-inflammatory activity of meloxicam. Importantly, the effects observed with the meloxicam-b-cyclodextrin complex are more pronounced compared to those of the free meloxicam. This observation may be relevant for developing new meloxicam preparations with increased bioavailability.