Third-generation solid dispersion combining Soluplus and poloxamer 407 enhances the oral bioavailability of resveratrol

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MetadadosDescriçãoIdioma
Autor(es): dc.contributorBIAL Portela & Ca SA-
Autor(es): dc.contributorUniv Porto-
Autor(es): dc.contributorUniversidade Estadual Paulista (Unesp)-
Autor(es): dc.contributorCESPU Inst Invest & Formacao Avancada Ciencias &-
Autor(es): dc.contributorInst Univ Ciencias Saude-
Autor(es): dc.creatorVasconcelos, Teofilo-
Autor(es): dc.creatorPrezotti, Fabiola [UNESP]-
Autor(es): dc.creatorAraujo, Francisca-
Autor(es): dc.creatorLopes, Carlos-
Autor(es): dc.creatorLoureiro, Ana-
Autor(es): dc.creatorMarques, Sara-
Autor(es): dc.creatorSarmento, Bruno-
Data de aceite: dc.date.accessioned2022-02-22T00:55:38Z-
Data de disponibilização: dc.date.available2022-02-22T00:55:38Z-
Data de envio: dc.date.issued2021-06-25-
Data de envio: dc.date.issued2021-06-25-
Data de envio: dc.date.issued2021-02-14-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.1016/j.ijpharm.2021.120245-
Fonte completa do material: dc.identifierhttp://hdl.handle.net/11449/209193-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/209193-
Descrição: dc.descriptionResveratrol is a very promising anti-oxidant drug candidate with low oral bioavailability due to its intrinsic poor water solubility, intestinal efflux and metabolization mechanisms. Resveratrol solubility high-throughput screening with different carriers was performed showing an enhancement above 2000-fold with Soluplus (R) and Tween (R) 80. The former was selected as a carrier at the ratio of resveratrol: Soluplus (R) (1:2). Then, third-generation solid dispersions were developed with Gelucire (R) and poloxamer 407 at 5 and 15% to resveratrol: Soluplus (R) (1:2). All formulations enhanced solubility around 2-fold when compared to resveratrol: Soluplus (R) (1:2) solid dispersion. Caco-2 cells permeability studies showed that both surfactants increased drug permeability and the fraction recovered (2-fold) suggesting that these could reduce efflux mechanism and metabolism. Formulation with 15% poloxamer 407 demonstrated most promising results and was selected for further studies. In in vivo studies, resveratrol:Soluplus (R): poloxamer 407 (1:2-15%) third generation solid dispersion presented an AUCo-t of 279 +/- 54 ng.h/mL and a Cmax of 134 +/- 78 ng/mL, 2.5 fold higher than solid dispersion without poloxamer 407. This work reports the development of third-generation solid dispersion that significantly improved resveratrol bioavailability. This was accomplished by an increased solubility and most probably by reducing intestinal efflux and metabolism mechanisms.-
Descrição: dc.descriptionFEDER - Fundo Europeu de Desenvolvimento Regional-
Descrição: dc.descriptionPortuguese funds through FCT - Fundacao para a Ciencia e a Tecnologia/Ministerio da Ciencia, Tecnologia e Ensino Superior-
Descrição: dc.descriptionBIAL Portela & Ca SA, Ave Siderugia Nacl, P-4745457 Trofa, Portugal-
Descrição: dc.descriptionUniv Porto, ICBAS Inst Ciencias Biomed Abel Salazar, Rua Jorge Viterbo Ferreira 228, P-4050313 Porto, Portugal-
Descrição: dc.descriptionUniv Porto, INEB Inst Engn Biomed, Rua Alfredo Allen 208, P-4200135 Porto, Portugal-
Descrição: dc.descriptionUniv Porto, i3S Inst Invest & Inovacao Saude, Rua Alfredo Allen 208, P-4200135 Porto, Portugal-
Descrição: dc.descriptionUniv Estadual Paulista, Fac Ciencias Farmaceut Araraquara Drugs & Pharmac, Sao Paulo, SP, Brazil-
Descrição: dc.descriptionUniv Porto, CIBIO InBIO UP Res Ctr Biodivers & Genet Resource, Rua Padre Armando Quintas 7, P-4485661 Vairao, Portugal-
Descrição: dc.descriptionCESPU Inst Invest & Formacao Avancada Ciencias &, Rua Cent Gandra 1317, P-4585116 Gandra, Portugal-
Descrição: dc.descriptionInst Univ Ciencias Saude, Rua Cent Gandra 1317, P-4585116 Gandra, Portugal-
Descrição: dc.descriptionUniv Estadual Paulista, Fac Ciencias Farmaceut Araraquara Drugs & Pharmac, Sao Paulo, SP, Brazil-
Descrição: dc.descriptionPortuguese funds through FCT - Fundacao para a Ciencia e a Tecnologia/Ministerio da Ciencia, Tecnologia e Ensino Superior: UID/BIM/04293/2019-
Descrição: dc.descriptionPortuguese funds through FCT - Fundacao para a Ciencia e a Tecnologia/Ministerio da Ciencia, Tecnologia e Ensino Superior: POCI-01-0145-FEDER-016385-
Formato: dc.format14-
Idioma: dc.languageen-
Publicador: dc.publisherElsevier B.V.-
Relação: dc.relationInternational Journal Of Pharmaceutics-
???dc.source???: dc.sourceWeb of Science-
Palavras-chave: dc.subjectSolid dispersions-
Palavras-chave: dc.subjectBioavailability-
Palavras-chave: dc.subjectAmorphous-
Palavras-chave: dc.subjectPermeability enhancer-
Palavras-chave: dc.subjectMetabolism inhibitor-
Palavras-chave: dc.subjectResveratrol-
Título: dc.titleThird-generation solid dispersion combining Soluplus and poloxamer 407 enhances the oral bioavailability of resveratrol-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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