Developing Transdermal Applications of Ketorolac Tromethamine Entrapped in Stimuli Sensitive Block Copolymer Hydrogels

Purpose: In order to obtain dermal vehicles of ketorolac tromethamine (KT) for the local treatment of inflammation and restrict undesirable side effects of systemic levels hydrogels (HGs) of poloxamer and carbomer were developed. Methods: KT poloxamer based HG (KT-P407-HG) and KT carbomer based HG (...

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Autores: Mallandrich Miret, Mireia, Fernández Campos, Francisco, Clares Naveros, Beatriz, Halbaut, Lyda, Alonso, Cristina, Coderch Negra, Ma. Luisa, Garduño Ramírez, María Luisa del Carmen, Andrade Carrera, Berenice, Pozo Carrascosa, Alfonso del, Lane, ME, Calpena Campmany, Ana Cristina
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2017
País:España
Institución:Universidad de Barcelona
Repositorio:Dipòsit Digital de la UB
OAI Identifier:oai:diposit.ub.edu:2445/128389
Acceso en línea:https://hdl.handle.net/2445/128389
Access Level:acceso abierto
Palabra clave:Farmacologia
Tecnologia farmacèutica
Administració de medicaments
Agents antiinflamatoris
Reologia
Fórmules magistrals
Medicació transdèrmica
Pharmacology
Pharmaceutical technology
Administration of drugs
Antiinflammatory agents
Rheology
Medical formularies
Transdermal medication
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spelling Developing Transdermal Applications of Ketorolac Tromethamine Entrapped in Stimuli Sensitive Block Copolymer HydrogelsMallandrich Miret, MireiaFernández Campos, FranciscoClares Naveros, BeatrizHalbaut, LydaAlonso, CristinaCoderch Negra, Ma. LuisaGarduño Ramírez, María Luisa del CarmenAndrade Carrera, BerenicePozo Carrascosa, Alfonso delLane, MECalpena Campmany, Ana CristinaFarmacologiaTecnologia farmacèuticaAdministració de medicamentsAgents antiinflamatorisReologiaFórmules magistralsMedicació transdèrmicaPharmacologyPharmaceutical technologyAdministration of drugsAntiinflammatory agentsRheologyMedical formulariesTransdermal medicationPurpose: In order to obtain dermal vehicles of ketorolac tromethamine (KT) for the local treatment of inflammation and restrict undesirable side effects of systemic levels hydrogels (HGs) of poloxamer and carbomer were developed. Methods: KT poloxamer based HG (KT-P407-HG) and KT carbomer based HG (KT-C940-HG) were elaborated and characterized in terms of swelling, degradation, porosity, rheology, stability, in vitro release, ex vivo permeation and distribution skin layers. Finally, in vivo anti-inflammatory efficacy and skin tolerance were also assessed. Results: HGs were transparent and kept stable after 3 months exhibiting biocompatible near neutral pH values. Rheological patterns fitted to Herschel-Bulkley for KT-C940-HG and Newton for KT-P407-HG due to its low viscosity at 25°C. Rapid release profiles were observed through first order kinetics. Following the surface the highest concentration of KT from C940-HG was found in the epidermis and the stratum corneum for P407-HG. Relevant anti-inflammatory efficacy of KT-P407-HG revealed enough ability to provide sufficient bioavailability KT to reach easily the site of action. The application of developed formulations in volunteers did not induce any visual skin irritation. Conclusions: KT-P407-HG was proposed as suitable formulation for anti-inflammatory local treatment without theoretical systemic side effect.Springer Science + Business Media2017info:eu-repo/semantics/articleinfo:eu-repo/semantics/acceptedVersionapplication/pdfhttps://hdl.handle.net/2445/128389Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)reponame:Dipòsit Digital de la UBinstname:Universidad de BarcelonaInglésVersió postprint del document publicat a: https://doi.org/10.1007/s11095-017-2181-8Pharmaceutical Research, 2017, vol. 34, num. 8, p. 1728-1740https://doi.org/10.1007/s11095-017-2181-8(c) Springer Science + Business Media, 2017info:eu-repo/semantics/openAccessoai:diposit.ub.edu:2445/1283892026-05-27T06:46:51Z
dc.title.none.fl_str_mv Developing Transdermal Applications of Ketorolac Tromethamine Entrapped in Stimuli Sensitive Block Copolymer Hydrogels
title Developing Transdermal Applications of Ketorolac Tromethamine Entrapped in Stimuli Sensitive Block Copolymer Hydrogels
spellingShingle Developing Transdermal Applications of Ketorolac Tromethamine Entrapped in Stimuli Sensitive Block Copolymer Hydrogels
Mallandrich Miret, Mireia
Farmacologia
Tecnologia farmacèutica
Administració de medicaments
Agents antiinflamatoris
Reologia
Fórmules magistrals
Medicació transdèrmica
Pharmacology
Pharmaceutical technology
Administration of drugs
Antiinflammatory agents
Rheology
Medical formularies
Transdermal medication
title_short Developing Transdermal Applications of Ketorolac Tromethamine Entrapped in Stimuli Sensitive Block Copolymer Hydrogels
title_full Developing Transdermal Applications of Ketorolac Tromethamine Entrapped in Stimuli Sensitive Block Copolymer Hydrogels
title_fullStr Developing Transdermal Applications of Ketorolac Tromethamine Entrapped in Stimuli Sensitive Block Copolymer Hydrogels
title_full_unstemmed Developing Transdermal Applications of Ketorolac Tromethamine Entrapped in Stimuli Sensitive Block Copolymer Hydrogels
title_sort Developing Transdermal Applications of Ketorolac Tromethamine Entrapped in Stimuli Sensitive Block Copolymer Hydrogels
dc.creator.none.fl_str_mv Mallandrich Miret, Mireia
Fernández Campos, Francisco
Clares Naveros, Beatriz
Halbaut, Lyda
Alonso, Cristina
Coderch Negra, Ma. Luisa
Garduño Ramírez, María Luisa del Carmen
Andrade Carrera, Berenice
Pozo Carrascosa, Alfonso del
Lane, ME
Calpena Campmany, Ana Cristina
author Mallandrich Miret, Mireia
author_facet Mallandrich Miret, Mireia
Fernández Campos, Francisco
Clares Naveros, Beatriz
Halbaut, Lyda
Alonso, Cristina
Coderch Negra, Ma. Luisa
Garduño Ramírez, María Luisa del Carmen
Andrade Carrera, Berenice
Pozo Carrascosa, Alfonso del
Lane, ME
Calpena Campmany, Ana Cristina
author_role author
author2 Fernández Campos, Francisco
Clares Naveros, Beatriz
Halbaut, Lyda
Alonso, Cristina
Coderch Negra, Ma. Luisa
Garduño Ramírez, María Luisa del Carmen
Andrade Carrera, Berenice
Pozo Carrascosa, Alfonso del
Lane, ME
Calpena Campmany, Ana Cristina
author2_role author
author
author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Farmacologia
Tecnologia farmacèutica
Administració de medicaments
Agents antiinflamatoris
Reologia
Fórmules magistrals
Medicació transdèrmica
Pharmacology
Pharmaceutical technology
Administration of drugs
Antiinflammatory agents
Rheology
Medical formularies
Transdermal medication
topic Farmacologia
Tecnologia farmacèutica
Administració de medicaments
Agents antiinflamatoris
Reologia
Fórmules magistrals
Medicació transdèrmica
Pharmacology
Pharmaceutical technology
Administration of drugs
Antiinflammatory agents
Rheology
Medical formularies
Transdermal medication
description Purpose: In order to obtain dermal vehicles of ketorolac tromethamine (KT) for the local treatment of inflammation and restrict undesirable side effects of systemic levels hydrogels (HGs) of poloxamer and carbomer were developed. Methods: KT poloxamer based HG (KT-P407-HG) and KT carbomer based HG (KT-C940-HG) were elaborated and characterized in terms of swelling, degradation, porosity, rheology, stability, in vitro release, ex vivo permeation and distribution skin layers. Finally, in vivo anti-inflammatory efficacy and skin tolerance were also assessed. Results: HGs were transparent and kept stable after 3 months exhibiting biocompatible near neutral pH values. Rheological patterns fitted to Herschel-Bulkley for KT-C940-HG and Newton for KT-P407-HG due to its low viscosity at 25°C. Rapid release profiles were observed through first order kinetics. Following the surface the highest concentration of KT from C940-HG was found in the epidermis and the stratum corneum for P407-HG. Relevant anti-inflammatory efficacy of KT-P407-HG revealed enough ability to provide sufficient bioavailability KT to reach easily the site of action. The application of developed formulations in volunteers did not induce any visual skin irritation. Conclusions: KT-P407-HG was proposed as suitable formulation for anti-inflammatory local treatment without theoretical systemic side effect.
publishDate 2017
dc.date.none.fl_str_mv 2017
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/acceptedVersion
format article
status_str acceptedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/2445/128389
url https://hdl.handle.net/2445/128389
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Versió postprint del document publicat a: https://doi.org/10.1007/s11095-017-2181-8
Pharmaceutical Research, 2017, vol. 34, num. 8, p. 1728-1740
https://doi.org/10.1007/s11095-017-2181-8
dc.rights.none.fl_str_mv (c) Springer Science + Business Media, 2017
info:eu-repo/semantics/openAccess
rights_invalid_str_mv (c) Springer Science + Business Media, 2017
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Springer Science + Business Media
publisher.none.fl_str_mv Springer Science + Business Media
dc.source.none.fl_str_mv Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)
reponame:Dipòsit Digital de la UB
instname:Universidad de Barcelona
instname_str Universidad de Barcelona
reponame_str Dipòsit Digital de la UB
collection Dipòsit Digital de la UB
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,301603

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