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
- Institución
- Consejo Nacional de Investigaciones Científicas y Técnicas
- OAI Identificador
- oai:ri.conicet.gov.ar:11336/77898
Ver los metadatos del registro completo
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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 Técnicas2025-09-29T09:50:21Zoai: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:34982025-09-29 09:50:21.484CONICET 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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1844613551887482880 |
score |
13.070432 |