Hydroxyzine, promethazine and thioridazine interaction with phospholipid monomolecular layers at the air-water interface

dc.creatorPinto, LDA
dc.creatorMalheiros, SVP
dc.creatorLino, ACS
dc.creatorde Paula, E
dc.creatorPerillo, MA
dc.date2006
dc.dateFEB 1
dc.date2014-11-14T04:46:26Z
dc.date2015-11-26T17:13:17Z
dc.date2014-11-14T04:46:26Z
dc.date2015-11-26T17:13:17Z
dc.date.accessioned2018-03-29T00:01:39Z
dc.date.available2018-03-29T00:01:39Z
dc.identifierBiophysical Chemistry. Elsevier Science Bv, v. 119, n. 3, n. 247, n. 255, 2006.
dc.identifier0301-4622
dc.identifier1873-4200
dc.identifierWOS:000235582500006
dc.identifier10.1016/j.bpc.2005.09.006
dc.identifierhttp://www.repositorio.unicamp.br/jspui/handle/REPOSIP/69045
dc.identifierhttp://www.repositorio.unicamp.br/handle/REPOSIP/69045
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/69045
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1281535
dc.descriptionIn this work the interaction of Hydroxyzine, Promethazine and Thioridazine with Langmuir films of dipalmitoylphosphatidylcholine (dpPC) and dipalmitoylphosphatidic acid (dpPA), is studied. Temporal variations in lateral surface pressure (pi) were measured at different initial pi (pi(i)), subphase pH and drug-concentration. Drugs with the smallest (PRO) and largest (HYD) molecular size exhibited the lowest adsorption (k(a)) and the highest desorption (k(d)) rate constant values, respectively. The affinity binding constants (K-b) obtained in monolayers followed the same profile (K-b,K-PRO<K-b,K-HYD<K-b,K-THI) of the egg-PC/water partition coefficients (P) determined in bilayers. The drug concentration required to reach the half-maximal Delta pi at pi(i)=14 mN/m (K-0.5), was very sensitive to pH. The maximal increment in pi upon drug incorporation into the monolayer will depend on the phospholipid collapse pressure (pi(c)), the monolayers's compressibility and drug's size, shape and charge. The higher pi(c) of dpPC lead to higher pi(cut-off) values (maximal pi allowing drug penetration), if compared with dpPA. In dpPC and dpPA pi(cut-off) decreased as a function of the molecular size of the uncharged drugs. In dpPA, protonated drugs became electrostatically trapped at the monolayer surface hence drug penetration, monolayer deformation and pi increase were impaired and the correlation between pi(cut-off) and drug molecular size was lost. (C) 2005 Elsevier B.V. All rights reserved.
dc.description119
dc.description3
dc.description247
dc.description255
dc.languageen
dc.publisherElsevier Science Bv
dc.publisherAmsterdam
dc.publisherHolanda
dc.relationBiophysical Chemistry
dc.relationBiophys. Chem.
dc.rightsfechado
dc.rightshttp://www.elsevier.com/about/open-access/open-access-policies/article-posting-policy
dc.sourceWeb of Science
dc.subjecthydroxyzine
dc.subjectpromethazine
dc.subjectthioridazine
dc.subjectLangmuir films
dc.subjectlateral surface pressure
dc.subjectphospholipids
dc.subjectSemisynthetic Derivatives
dc.subjectLateral Pressure
dc.subjectFlunitrazepam
dc.subjectMonolayers
dc.subjectMembranes
dc.subjectSphingosine
dc.subjectBilayers
dc.subjectBinding
dc.titleHydroxyzine, promethazine and thioridazine interaction with phospholipid monomolecular layers at the air-water interface
dc.typeArtículos de revistas


Este ítem pertenece a la siguiente institución