Novel transdermal bioadhesive surfactant-based system for release and solubility improvement of antimalarial drugs artemether-lumefantrine

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Autor(es): dc.contributorUniversity at Campinas-
Autor(es): dc.contributorQueen's University Belfast-
Autor(es): dc.contributorUniversidade Estadual Paulista (UNESP)-
Autor(es): dc.contributor3D Printing Open Lab - Laprint-
Autor(es): dc.contributorInstituto de Biociencias-
Autor(es): dc.contributorUniversidade Estadual de Campinas (UNICAMP)-
Autor(es): dc.contributorUniversity of Calabar-
Autor(es): dc.creatorVolpe-Zanutto, Fabiana-
Autor(es): dc.creatorFonseca-Santos, Bruno-
Autor(es): dc.creatorMcKenna, Peter E.-
Autor(es): dc.creatorParedes, Alejandro J-
Autor(es): dc.creatorDávila, José Luis-
Autor(es): dc.creatorMcCrudden, Maelíosa T. C.-
Autor(es): dc.creatorTangerina, Marcelo Marucci Pereira-
Autor(es): dc.creatorCeccheto Figueiredo, Mariana-
Autor(es): dc.creatorVilegas, Wagner-
Autor(es): dc.creatorBrisibe, Andi-
Autor(es): dc.creatorAkira D'vila, Marcos-
Autor(es): dc.creatorDonnelly, Ryan F.-
Autor(es): dc.creatorChorilli, Marlus-
Autor(es): dc.creatorFoglio, Mary Ann-
Data de aceite: dc.date.accessioned2025-08-21T18:30:52Z-
Data de disponibilização: dc.date.available2025-08-21T18:30:52Z-
Data de envio: dc.date.issued2022-04-29-
Data de envio: dc.date.issued2022-04-29-
Data de envio: dc.date.issued2021-10-31-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.1088/1748-605X/ac2885-
Fonte completa do material: dc.identifierhttp://hdl.handle.net/11449/229721-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/229721-
Descrição: dc.descriptionArtemether (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.-
Descrição: dc.descriptionGraduate School of Bioscience and Technology of Bioactive Products Biology Institute University at Campinas, Sao Paulo-
Descrição: dc.descriptionSchool of Pharmacy Queen's University Belfast-
Descrição: dc.descriptionUNESP- University Estadual Paulista Faculdade de Ciencias Farmaceuticas UNESP, Sao Paulo-
Descrição: dc.descriptionFaculty of Pharmaceutical Science University at Campinas, Sao Paulo-
Descrição: dc.descriptionCentre for Information Technology 'Renato Archer' (CTI) 3D Printing Open Lab - Laprint, Sao Paulo-
Descrição: dc.descriptionUniversidade de S o Paulo Departamento de Bot nica Instituto de Biociencias, Sao Paulo-
Descrição: dc.descriptionFaculdade de Ciencias Médicas Universidade Estadual de Campinas, Sao Paulo-
Descrição: dc.descriptionSchool of Mechanical Engineering University of Campinas, Sao Paulo-
Descrição: dc.descriptionUNESP Univ Estadual Paulista Instituto de Biociencias, Sao Vicente-
Descrição: dc.descriptionUniversity of Calabar-
Descrição: dc.descriptionUNESP- University Estadual Paulista Faculdade de Ciencias Farmaceuticas UNESP, Sao Paulo-
Descrição: dc.descriptionUNESP Univ Estadual Paulista Instituto de Biociencias, Sao Vicente-
Idioma: dc.languageen-
Relação: dc.relationBiomedical Materials (Bristol)-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subjectartemether-
Palavras-chave: dc.subjectlumefantrine-
Palavras-chave: dc.subjectmalaria-
Palavras-chave: dc.subjectsurfactant-based system-
Palavras-chave: dc.subjecttransdermal-
Título: dc.titleNovel transdermal bioadhesive surfactant-based system for release and solubility improvement of antimalarial drugs artemether-lumefantrine-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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