Novel transdermal bioadhesive surfactant-based system for release and solubility improvement of antimalarial drugs artemether-lumefantrine
Autor(a) principal: | |
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Data de Publicação: | 2021 |
Outros Autores: | , , , , , , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.1088/1748-605X/ac2885 http://hdl.handle.net/11449/229721 |
Resumo: | Artemether (ART) and lumefantrine (LUM) are the gold standard antimalarial drugs used for the treatment of malaria in children and pregnant women. Typically, ART and LUM are delivered orally in the form of a combined tablet, however, the appropriateness of this route of administration for these drugs is questionable due to the poor absorption and therefore bioavailability observed unless administered alongside lipid-rich foods. Transdermal drug delivery in the form of a patch-type system has been identified as a viable alternative to the conventional tablet-based therapy. A novel, surfactant-based ART-LUM formulation (S3AL), developed for transdermal delivery, may eliminate the shortcomings associated with oral delivery; namely poor drug absorption which is caused by the inherently low solubility of ART and LUM. Moreover, by successfully delivering these antimalarials transdermally, first-pass metabolism will be avoided leading to enhanced drug bioavailability in both cases. The S3AL formulation contained ART and LUM at equal concentrations (2.5% w/w of each) as well as Procetyl® AWS (30% w/w), oleic acid (10% w/w), 1-methyl-2-pyrrolidone (10% w/w), and water (45% w/w). The addition of LUM to the formulation changed the system from a striae structure to a dark field structure when visualized by a polarized light microscope. Additionally, this system possessed higher viscosity and superior skin bioadhesion, as evidenced by mechanical characterization, when compared to a similar formulation containing ART alone. S3AL was also proven to be biocompatible to human keratinocyte cells. Finally, in vitro studies demonstrated the propensity of S3AL for successful delivery via the transdermal route, with 2279 295 µg cm-2 of ART and 94 13 µg cm-2 of LUM having permeated across dermatomed porcine skin after 24 h, highlighting its potential as a new candidate for the treatment of malaria. |
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Novel transdermal bioadhesive surfactant-based system for release and solubility improvement of antimalarial drugs artemether-lumefantrineartemetherlumefantrinemalariasurfactant-based systemtransdermalArtemether (ART) and lumefantrine (LUM) are the gold standard antimalarial drugs used for the treatment of malaria in children and pregnant women. Typically, ART and LUM are delivered orally in the form of a combined tablet, however, the appropriateness of this route of administration for these drugs is questionable due to the poor absorption and therefore bioavailability observed unless administered alongside lipid-rich foods. Transdermal drug delivery in the form of a patch-type system has been identified as a viable alternative to the conventional tablet-based therapy. A novel, surfactant-based ART-LUM formulation (S3AL), developed for transdermal delivery, may eliminate the shortcomings associated with oral delivery; namely poor drug absorption which is caused by the inherently low solubility of ART and LUM. Moreover, by successfully delivering these antimalarials transdermally, first-pass metabolism will be avoided leading to enhanced drug bioavailability in both cases. The S3AL formulation contained ART and LUM at equal concentrations (2.5% w/w of each) as well as Procetyl® AWS (30% w/w), oleic acid (10% w/w), 1-methyl-2-pyrrolidone (10% w/w), and water (45% w/w). The addition of LUM to the formulation changed the system from a striae structure to a dark field structure when visualized by a polarized light microscope. Additionally, this system possessed higher viscosity and superior skin bioadhesion, as evidenced by mechanical characterization, when compared to a similar formulation containing ART alone. S3AL was also proven to be biocompatible to human keratinocyte cells. Finally, in vitro studies demonstrated the propensity of S3AL for successful delivery via the transdermal route, with 2279 295 µg cm-2 of ART and 94 13 µg cm-2 of LUM having permeated across dermatomed porcine skin after 24 h, highlighting its potential as a new candidate for the treatment of malaria.Graduate School of Bioscience and Technology of Bioactive Products Biology Institute University at Campinas, Sao PauloSchool of Pharmacy Queen's University BelfastUNESP- University Estadual Paulista Faculdade de Ciencias Farmaceuticas UNESP, Sao PauloFaculty of Pharmaceutical Science University at Campinas, Sao PauloCentre for Information Technology 'Renato Archer' (CTI) 3D Printing Open Lab - Laprint, Sao PauloUniversidade de S o Paulo Departamento de Bot nica Instituto de Biociencias, Sao PauloFaculdade de Ciencias Médicas Universidade Estadual de Campinas, Sao PauloSchool of Mechanical Engineering University of Campinas, Sao PauloUNESP Univ Estadual Paulista Instituto de Biociencias, Sao VicenteUniversity of CalabarUNESP- University Estadual Paulista Faculdade de Ciencias Farmaceuticas UNESP, Sao PauloUNESP Univ Estadual Paulista Instituto de Biociencias, Sao VicenteUniversity at CampinasQueen's University BelfastUniversidade Estadual Paulista (UNESP)3D Printing Open Lab - LaprintInstituto de BiocienciasUniversidade Estadual de Campinas (UNICAMP)University of CalabarVolpe-Zanutto, FabianaFonseca-Santos, Bruno [UNESP]McKenna, Peter E.Paredes, Alejandro JDávila, José LuisMcCrudden, Maelíosa T. C.Tangerina, Marcelo Marucci PereiraCeccheto Figueiredo, MarianaVilegas, Wagner [UNESP]Brisibe, AndiAkira D'vila, MarcosDonnelly, Ryan F.Chorilli, Marlus [UNESP]Foglio, Mary Ann2022-04-29T08:35:30Z2022-04-29T08:35:30Z2021-11-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://dx.doi.org/10.1088/1748-605X/ac2885Biomedical Materials (Bristol), v. 16, n. 6, 2021.1748-605X1748-6041http://hdl.handle.net/11449/22972110.1088/1748-605X/ac28852-s2.0-85117235799Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengBiomedical Materials (Bristol)info:eu-repo/semantics/openAccess2022-04-29T08:35:30Zoai:repositorio.unesp.br:11449/229721Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T17:53:29.860066Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Novel transdermal bioadhesive surfactant-based system for release and solubility improvement of antimalarial drugs artemether-lumefantrine |
title |
Novel transdermal bioadhesive surfactant-based system for release and solubility improvement of antimalarial drugs artemether-lumefantrine |
spellingShingle |
Novel transdermal bioadhesive surfactant-based system for release and solubility improvement of antimalarial drugs artemether-lumefantrine Volpe-Zanutto, Fabiana artemether lumefantrine malaria surfactant-based system transdermal |
title_short |
Novel transdermal bioadhesive surfactant-based system for release and solubility improvement of antimalarial drugs artemether-lumefantrine |
title_full |
Novel transdermal bioadhesive surfactant-based system for release and solubility improvement of antimalarial drugs artemether-lumefantrine |
title_fullStr |
Novel transdermal bioadhesive surfactant-based system for release and solubility improvement of antimalarial drugs artemether-lumefantrine |
title_full_unstemmed |
Novel transdermal bioadhesive surfactant-based system for release and solubility improvement of antimalarial drugs artemether-lumefantrine |
title_sort |
Novel transdermal bioadhesive surfactant-based system for release and solubility improvement of antimalarial drugs artemether-lumefantrine |
author |
Volpe-Zanutto, Fabiana |
author_facet |
Volpe-Zanutto, Fabiana Fonseca-Santos, Bruno [UNESP] McKenna, Peter E. Paredes, Alejandro J Dávila, José Luis McCrudden, Maelíosa T. C. Tangerina, Marcelo Marucci Pereira Ceccheto Figueiredo, Mariana Vilegas, Wagner [UNESP] Brisibe, Andi Akira D'vila, Marcos Donnelly, Ryan F. Chorilli, Marlus [UNESP] Foglio, Mary Ann |
author_role |
author |
author2 |
Fonseca-Santos, Bruno [UNESP] McKenna, Peter E. Paredes, Alejandro J Dávila, José Luis McCrudden, Maelíosa T. C. Tangerina, Marcelo Marucci Pereira Ceccheto Figueiredo, Mariana Vilegas, Wagner [UNESP] Brisibe, Andi Akira D'vila, Marcos Donnelly, Ryan F. Chorilli, Marlus [UNESP] Foglio, Mary Ann |
author2_role |
author author author author author author author author author author author author author |
dc.contributor.none.fl_str_mv |
University at Campinas Queen's University Belfast Universidade Estadual Paulista (UNESP) 3D Printing Open Lab - Laprint Instituto de Biociencias Universidade Estadual de Campinas (UNICAMP) University of Calabar |
dc.contributor.author.fl_str_mv |
Volpe-Zanutto, Fabiana Fonseca-Santos, Bruno [UNESP] McKenna, Peter E. Paredes, Alejandro J Dávila, José Luis McCrudden, Maelíosa T. C. Tangerina, Marcelo Marucci Pereira Ceccheto Figueiredo, Mariana Vilegas, Wagner [UNESP] Brisibe, Andi Akira D'vila, Marcos Donnelly, Ryan F. Chorilli, Marlus [UNESP] Foglio, Mary Ann |
dc.subject.por.fl_str_mv |
artemether lumefantrine malaria surfactant-based system transdermal |
topic |
artemether lumefantrine malaria surfactant-based system transdermal |
description |
Artemether (ART) and lumefantrine (LUM) are the gold standard antimalarial drugs used for the treatment of malaria in children and pregnant women. Typically, ART and LUM are delivered orally in the form of a combined tablet, however, the appropriateness of this route of administration for these drugs is questionable due to the poor absorption and therefore bioavailability observed unless administered alongside lipid-rich foods. Transdermal drug delivery in the form of a patch-type system has been identified as a viable alternative to the conventional tablet-based therapy. A novel, surfactant-based ART-LUM formulation (S3AL), developed for transdermal delivery, may eliminate the shortcomings associated with oral delivery; namely poor drug absorption which is caused by the inherently low solubility of ART and LUM. Moreover, by successfully delivering these antimalarials transdermally, first-pass metabolism will be avoided leading to enhanced drug bioavailability in both cases. The S3AL formulation contained ART and LUM at equal concentrations (2.5% w/w of each) as well as Procetyl® AWS (30% w/w), oleic acid (10% w/w), 1-methyl-2-pyrrolidone (10% w/w), and water (45% w/w). The addition of LUM to the formulation changed the system from a striae structure to a dark field structure when visualized by a polarized light microscope. Additionally, this system possessed higher viscosity and superior skin bioadhesion, as evidenced by mechanical characterization, when compared to a similar formulation containing ART alone. S3AL was also proven to be biocompatible to human keratinocyte cells. Finally, in vitro studies demonstrated the propensity of S3AL for successful delivery via the transdermal route, with 2279 295 µg cm-2 of ART and 94 13 µg cm-2 of LUM having permeated across dermatomed porcine skin after 24 h, highlighting its potential as a new candidate for the treatment of malaria. |
publishDate |
2021 |
dc.date.none.fl_str_mv |
2021-11-01 2022-04-29T08:35:30Z 2022-04-29T08:35:30Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://dx.doi.org/10.1088/1748-605X/ac2885 Biomedical Materials (Bristol), v. 16, n. 6, 2021. 1748-605X 1748-6041 http://hdl.handle.net/11449/229721 10.1088/1748-605X/ac2885 2-s2.0-85117235799 |
url |
http://dx.doi.org/10.1088/1748-605X/ac2885 http://hdl.handle.net/11449/229721 |
identifier_str_mv |
Biomedical Materials (Bristol), v. 16, n. 6, 2021. 1748-605X 1748-6041 10.1088/1748-605X/ac2885 2-s2.0-85117235799 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Biomedical Materials (Bristol) |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.source.none.fl_str_mv |
Scopus reponame:Repositório Institucional da UNESP instname:Universidade Estadual Paulista (UNESP) instacron:UNESP |
instname_str |
Universidade Estadual Paulista (UNESP) |
instacron_str |
UNESP |
institution |
UNESP |
reponame_str |
Repositório Institucional da UNESP |
collection |
Repositório Institucional da UNESP |
repository.name.fl_str_mv |
Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP) |
repository.mail.fl_str_mv |
|
_version_ |
1808128873006628864 |