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

Autores
Pinto, Luciana de Matos Alves; Malheiros, Sônia Valéria Pinheiro; Lino, Antônio Carlos Senges; de Paula, Eneida; Perillo, Maria Angelica
Año de publicación
2006
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
In 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 (π) were measured at different initial π (πi), 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 (kd) rate constant values, respectively. The affinity binding constants (Kb) obtained in monolayers followed the same profile (Kb,PRO < Kb,HYD < Kb,THI) of the egg-PC/water partition coefficients (P) determined in bilayers. The drug concentration required to reach the half-maximal Δπ at πi = 14 mN/m (K0.5), was very sensitive to pH. The maximal increment in π upon drug incorporation into the monolayer (Δπmax) will depend on the phospholipid collapse pressure (πc), the monolayers's compressibility and drug's size, shape and charge. The higher πc of dpPC lead to higher πcut-off values (maximal π allowing drug penetration), if compared with dpPA. In dpPC and dpPA πcut-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 π increase were impaired and the correlation between πcut-off and drug molecular size was lost. © 2005 Elsevier B.V. All rights reserved.
Fil: Pinto, Luciana de Matos Alves. Universidade Estadual de Campinas; Brasil
Fil: Malheiros, Sônia Valéria Pinheiro. Universidade Estadual de Campinas; Brasil
Fil: Lino, Antônio Carlos Senges. Universidade Estadual de Campinas; Brasil
Fil: de Paula, Eneida. Universidade Estadual de Campinas; Brasil
Fil: Perillo, Maria Angelica. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; Argentina
Materia
Hydroxyzine
Langmuir Films
Lateral Surface Pressure
Phospholipids
Promethazine
Thioridazine
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/77898
Acceder
id CONICETDig_4f9e143e24a81440b84d43385f483150
oai_identifier_str oai:ri.conicet.gov.ar:11336/77898
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Hydroxyzine, promethazine and thioridazine interaction with phospholipid monomolecular layers at the air-water interfacePinto, Luciana de Matos AlvesMalheiros, Sônia Valéria PinheiroLino, Antônio Carlos Sengesde Paula, EneidaPerillo, Maria AngelicaHydroxyzineLangmuir FilmsLateral Surface PressurePhospholipidsPromethazineThioridazinehttps://purl.org/becyt/ford/1.6https://purl.org/becyt/ford/1In 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 (π) were measured at different initial π (πi), 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 (kd) rate constant values, respectively. The affinity binding constants (Kb) obtained in monolayers followed the same profile (Kb,PRO < Kb,HYD < Kb,THI) of the egg-PC/water partition coefficients (P) determined in bilayers. The drug concentration required to reach the half-maximal Δπ at πi = 14 mN/m (K0.5), was very sensitive to pH. The maximal increment in π upon drug incorporation into the monolayer (Δπmax) will depend on the phospholipid collapse pressure (πc), the monolayers's compressibility and drug's size, shape and charge. The higher πc of dpPC lead to higher πcut-off values (maximal π allowing drug penetration), if compared with dpPA. In dpPC and dpPA πcut-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 π increase were impaired and the correlation between πcut-off and drug molecular size was lost. © 2005 Elsevier B.V. All rights reserved.Fil: Pinto, Luciana de Matos Alves. Universidade Estadual de Campinas; BrasilFil: Malheiros, Sônia Valéria Pinheiro. Universidade Estadual de Campinas; BrasilFil: Lino, Antônio Carlos Senges. Universidade Estadual de Campinas; BrasilFil: de Paula, Eneida. Universidade Estadual de Campinas; BrasilFil: Perillo, Maria Angelica. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; ArgentinaElsevier Science2006-02-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/77898Pinto, Luciana de Matos Alves; Malheiros, Sônia Valéria Pinheiro; Lino, Antônio Carlos Senges; de Paula, Eneida; Perillo, Maria Angelica; Hydroxyzine, promethazine and thioridazine interaction with phospholipid monomolecular layers at the air-water interface; Elsevier Science; Biophysical Chemistry; 119; 3; 1-2-2006; 247-2550301-4622CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/pii/S0301462205002176info:eu-repo/semantics/altIdentifier/doi/10.1016/j.bpc.2005.09.006info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-10-22T11:19:41Zoai:ri.conicet.gov.ar:11336/77898instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-10-22 11:19:41.646CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Hydroxyzine, promethazine and thioridazine interaction with phospholipid monomolecular layers at the air-water interface
title Hydroxyzine, promethazine and thioridazine interaction with phospholipid monomolecular layers at the air-water interface
spellingShingle Hydroxyzine, promethazine and thioridazine interaction with phospholipid monomolecular layers at the air-water interface
Pinto, Luciana de Matos Alves
Hydroxyzine
Langmuir Films
Lateral Surface Pressure
Phospholipids
Promethazine
Thioridazine
title_short Hydroxyzine, promethazine and thioridazine interaction with phospholipid monomolecular layers at the air-water interface
title_full Hydroxyzine, promethazine and thioridazine interaction with phospholipid monomolecular layers at the air-water interface
title_fullStr Hydroxyzine, promethazine and thioridazine interaction with phospholipid monomolecular layers at the air-water interface
title_full_unstemmed Hydroxyzine, promethazine and thioridazine interaction with phospholipid monomolecular layers at the air-water interface
title_sort Hydroxyzine, promethazine and thioridazine interaction with phospholipid monomolecular layers at the air-water interface
dc.creator.none.fl_str_mv Pinto, Luciana de Matos Alves
Malheiros, Sônia Valéria Pinheiro
Lino, Antônio Carlos Senges
de Paula, Eneida
Perillo, Maria Angelica
author Pinto, Luciana de Matos Alves
author_facet Pinto, Luciana de Matos Alves
Malheiros, Sônia Valéria Pinheiro
Lino, Antônio Carlos Senges
de Paula, Eneida
Perillo, Maria Angelica
author_role author
author2 Malheiros, Sônia Valéria Pinheiro
Lino, Antônio Carlos Senges
de Paula, Eneida
Perillo, Maria Angelica
author2_role author
author
author
author
dc.subject.none.fl_str_mv Hydroxyzine
Langmuir Films
Lateral Surface Pressure
Phospholipids
Promethazine
Thioridazine
topic Hydroxyzine
Langmuir Films
Lateral Surface Pressure
Phospholipids
Promethazine
Thioridazine
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.6
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv In 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 (π) were measured at different initial π (πi), 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 (kd) rate constant values, respectively. The affinity binding constants (Kb) obtained in monolayers followed the same profile (Kb,PRO < Kb,HYD < Kb,THI) of the egg-PC/water partition coefficients (P) determined in bilayers. The drug concentration required to reach the half-maximal Δπ at πi = 14 mN/m (K0.5), was very sensitive to pH. The maximal increment in π upon drug incorporation into the monolayer (Δπmax) will depend on the phospholipid collapse pressure (πc), the monolayers's compressibility and drug's size, shape and charge. The higher πc of dpPC lead to higher πcut-off values (maximal π allowing drug penetration), if compared with dpPA. In dpPC and dpPA πcut-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 π increase were impaired and the correlation between πcut-off and drug molecular size was lost. © 2005 Elsevier B.V. All rights reserved.
Fil: Pinto, Luciana de Matos Alves. Universidade Estadual de Campinas; Brasil
Fil: Malheiros, Sônia Valéria Pinheiro. Universidade Estadual de Campinas; Brasil
Fil: Lino, Antônio Carlos Senges. Universidade Estadual de Campinas; Brasil
Fil: de Paula, Eneida. Universidade Estadual de Campinas; Brasil
Fil: Perillo, Maria Angelica. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; Argentina
description In 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 (π) were measured at different initial π (πi), 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 (kd) rate constant values, respectively. The affinity binding constants (Kb) obtained in monolayers followed the same profile (Kb,PRO < Kb,HYD < Kb,THI) of the egg-PC/water partition coefficients (P) determined in bilayers. The drug concentration required to reach the half-maximal Δπ at πi = 14 mN/m (K0.5), was very sensitive to pH. The maximal increment in π upon drug incorporation into the monolayer (Δπmax) will depend on the phospholipid collapse pressure (πc), the monolayers's compressibility and drug's size, shape and charge. The higher πc of dpPC lead to higher πcut-off values (maximal π allowing drug penetration), if compared with dpPA. In dpPC and dpPA πcut-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 π increase were impaired and the correlation between πcut-off and drug molecular size was lost. © 2005 Elsevier B.V. All rights reserved.
publishDate 2006
dc.date.none.fl_str_mv 2006-02-01
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/77898
Pinto, Luciana de Matos Alves; Malheiros, Sônia Valéria Pinheiro; Lino, Antônio Carlos Senges; de Paula, Eneida; Perillo, Maria Angelica; Hydroxyzine, promethazine and thioridazine interaction with phospholipid monomolecular layers at the air-water interface; Elsevier Science; Biophysical Chemistry; 119; 3; 1-2-2006; 247-255
0301-4622
CONICET Digital
CONICET
url http://hdl.handle.net/11336/77898
identifier_str_mv Pinto, Luciana de Matos Alves; Malheiros, Sônia Valéria Pinheiro; Lino, Antônio Carlos Senges; de Paula, Eneida; Perillo, Maria Angelica; Hydroxyzine, promethazine and thioridazine interaction with phospholipid monomolecular layers at the air-water interface; Elsevier Science; Biophysical Chemistry; 119; 3; 1-2-2006; 247-255
0301-4622
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/pii/S0301462205002176
info:eu-repo/semantics/altIdentifier/doi/10.1016/j.bpc.2005.09.006
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Elsevier Science
publisher.none.fl_str_mv Elsevier Science
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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score 12.982451

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