Enhanced geranylgeraniol stability and dissolution from self-emulsifying pellets containing the sucupira (Pterodon emarginatus Vogel) standardized extract

Detalhes bibliográficos
Autor(a) principal: Alves, Suzana Ferreira
Data de Publicação: 2023
Outros Autores: Marreto, Ricardo Neves, Bara, Maria Teresa Freitas
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Research, Society and Development
Texto Completo: https://rsdjournal.org/index.php/rsd/article/view/41314
Resumo: The vegetal species sucupira (Pterodon emarginatus Vogel) presents some diterpenes that have anti-inflammatory activities. However, diterpenes are poorly water-soluble compounds. The development of Self-Emulsifying Drug Delivery Systems (SEDDS) allows for obtaining a solid dosage form that maximizes the release of P. emarginatus constituents in an aqueous medium. This work aimed to obtain and characterize pellets containing the SEDDS prepared from P. emarginatus extract using the extrusion-spheronization technique. Formulations PF1 to PF6 were tested. Then, self-emulsifying formulations were prepared (SES1 to SES5) based on the mixture of poloxamer 188 (Pluronic® F-68) and sorbitan triolate (Span®85) with P. emarginatus extract. Next, formulation PF6, containing microcrystalline cellulose: P. emargitus extract: aerosil®200: polyvinylpyrrolindone K-30 (50: 54.25: 4: 4) was used in the preparation of pellets containing the self-emulsifying systems. These pellets had a homogeneous surface and average sphericity of 0.52. When encapsulated in hard gelatin capsules, it was noted that the formulations PF6, PSES3 and PSES4 were statistically different from each other at the 5% level. In the first 10 min of dissolution, PSES3 and PSES4 showed a higher level of geranylgeraniol released compared to the PF6 (p=0.000117). However, after 20 min of dissolution, no significant difference was observed in relation to the content of this compound. In the accelerated stability study, the average content of the geranylgeraniol was 85.6% and 81.8% for PSES3 and PSES4, respectively, whereas it was only 34.4% for PF6. Under the studied conditions, obtaining the self-emulsifying systems made it possible to achieve the desired dissolution and chemical stability of geranylgeraniol.
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spelling Enhanced geranylgeraniol stability and dissolution from self-emulsifying pellets containing the sucupira (Pterodon emarginatus Vogel) standardized extract Dissolución e estabilidad mejoradas de geranilgeraniol en péletes autoemulsionantes que contienen el extracto estandarizado de sucupira (Pterodon emarginatus Vogel)Dissolução e estabilidade aprimoradas do geranilgeraniol em pellets autoemulsionáveis contendo o extrato padronizado de sucupira (Pterodon emarginatus Vogel)Plantas medicinaisBioprodutosTecnologia fitofarmacêuticaSEDDS. Plantas medicinalesBioproductosTecnología farmacéuticaSEDDS.BioproductsPhytopharmaceutical technologyMedicinal plantsSEDDS. The vegetal species sucupira (Pterodon emarginatus Vogel) presents some diterpenes that have anti-inflammatory activities. However, diterpenes are poorly water-soluble compounds. The development of Self-Emulsifying Drug Delivery Systems (SEDDS) allows for obtaining a solid dosage form that maximizes the release of P. emarginatus constituents in an aqueous medium. This work aimed to obtain and characterize pellets containing the SEDDS prepared from P. emarginatus extract using the extrusion-spheronization technique. Formulations PF1 to PF6 were tested. Then, self-emulsifying formulations were prepared (SES1 to SES5) based on the mixture of poloxamer 188 (Pluronic® F-68) and sorbitan triolate (Span®85) with P. emarginatus extract. Next, formulation PF6, containing microcrystalline cellulose: P. emargitus extract: aerosil®200: polyvinylpyrrolindone K-30 (50: 54.25: 4: 4) was used in the preparation of pellets containing the self-emulsifying systems. These pellets had a homogeneous surface and average sphericity of 0.52. When encapsulated in hard gelatin capsules, it was noted that the formulations PF6, PSES3 and PSES4 were statistically different from each other at the 5% level. In the first 10 min of dissolution, PSES3 and PSES4 showed a higher level of geranylgeraniol released compared to the PF6 (p=0.000117). However, after 20 min of dissolution, no significant difference was observed in relation to the content of this compound. In the accelerated stability study, the average content of the geranylgeraniol was 85.6% and 81.8% for PSES3 and PSES4, respectively, whereas it was only 34.4% for PF6. Under the studied conditions, obtaining the self-emulsifying systems made it possible to achieve the desired dissolution and chemical stability of geranylgeraniol.La especie vegetal sucupira (Pterodon emarginatus Vogel)  presenta algunos diterpenos que tienen  actividades antiinflamatorias. Sin embargo, los diterpenos son compuestos poco solubles en agua. El desarrollo de sistemas de administración de fármacos autoemulsionantes (SEDDS) permite obtener una forma farmacéutica sólida que maximiza la liberación de los constituyentes de P. emarginatus en un medio acuoso.  Este trabajo pretendia obtener y caracterizar pellets que contengan SEDDS preparados a partir del extracto de P. emarginatus. Se probaron las formulaciones PF1 a PF6. Luego, se prepararon formulaciones autoemulsionantes (SES1 a SES5) a base de la mezcla de poloxámero 188 (Pluronic® F-68) y trilato de sorbitán (Span®85) con extracto. Posteriormente, la formulación de PF6, que contiene celulosa microcristalina: extracto de P. emargitus: aerosil®200: polivinilpirrolindona K-30 (50: 54,25: 4: 4), se utilizó en la preparación de gránulos que contenían los sistemas autoemulsionantes. Cuando se encapsuló en cápsulas de gelatina dura, se observó que las formulaciones de PF6, PSES3 y PSES4 fueron estadísticamente diferentes entre sí al nivel del 5%. En los primeros 10 min de disolución, PSES3 y PSES4 demostraron una mayor liberación de geranilgeraniol en comparación con PF6 (p=0,000117). Sin embargo, luego de 20 min de disolución, no se observó diferencia significativa en relación al contenido de este compuesto. En el estudio de estabilidad acelerada, el contenido medio de geranilgeraniol fue de 85,6% y 81,8% para PSES3 y PSES4, respectivamente, mientras que para PF6 fue solo de 34,4%. En las condiciones estudiadas, la obtención de sistemas autoemulsionantes permitió obtener la disolución y estabilidad química deseadas del geranilgeraniol.A espécie vegetal sucupira (Pterodon emarginatus Vogel) apresenta alguns diterpenos que possuem atividades anti-inflamatórias. No entanto, os diterpenos são compostos pouco solúveis em água. O desenvolvimento de sistemas de liberação de fármacos autoemulsionáveis (SEDDS) permite a obtenção de uma forma farmacêutica sólida que maximize a liberação de constituintes de P. emarginatus em meio aquoso. Este trabalho visou obter e caracterizar pellets contendo SEDDS preparados a partir do extrato de P. emarginatus pela técnica de extrusão-esferonização. As formulações PF1 a PF6 foram testadas. Em seguida, formulações autoemulsionáveis foram preparadas (SES1 a SES5) com base na mistura de poloxamer 188 (Pluronic® F-68) e triolato de sorbitano (Span®85) com extrato de P. emarginatus. Posteriormente, a formulação PF6, contendo celulose microcristalina: extrato de P. emargitus: aerosil®200: polivinilpirrolindona K-30 (50: 54,25: 4: 4) foi utilizada na preparação dos pellets contendo os sistemas autoemulsionáveis. Esses pellets apresentaram superfície homogênea e esfericidade média de 0,52. Quando encapsulado em cápsulas de gelatina dura notou-se que as formulações PF6, PSES3 e PSES4 foram estatisticamente diferentes entre si ao nível de 5%. Nos primeiros 10 min de dissolução, PSES3 e PSES4 demonstraram uma maior liberação de geranilgeraniol comparado à PF6 (p=0.000117). Porém, após 20 min de dissolução, nenhuma diferença significativa foi observada em relação ao conteúdo desse composto. No estudo de estabilidade acelerada, o teor médio do geranilgeraniol foi de 85,6% e 81,8% para PSES3 e PSES4, respectivamente, enquanto foi de apenas 34,4% para PF6. Nas condições estudadas, a obtenção dos sistemas autoemulsificantes possibilitou a obtenção da dissolução e estabilidade química desejadas do geranilgeraniol.Research, Society and Development2023-04-18info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://rsdjournal.org/index.php/rsd/article/view/4131410.33448/rsd-v12i4.41314Research, Society and Development; Vol. 12 No. 4; e26012441314Research, Society and Development; Vol. 12 Núm. 4; e26012441314Research, Society and Development; v. 12 n. 4; e260124413142525-3409reponame:Research, Society and Developmentinstname:Universidade Federal de Itajubá (UNIFEI)instacron:UNIFEIenghttps://rsdjournal.org/index.php/rsd/article/view/41314/33588Copyright (c) 2023 Suzana Ferreira Alves; Ricardo Neves Marreto; Maria Teresa Freitas Barahttps://creativecommons.org/licenses/by/4.0info:eu-repo/semantics/openAccessAlves, Suzana Ferreira Marreto, Ricardo Neves Bara, Maria Teresa Freitas 2023-04-21T18:13:32Zoai:ojs.pkp.sfu.ca:article/41314Revistahttps://rsdjournal.org/index.php/rsd/indexPUBhttps://rsdjournal.org/index.php/rsd/oairsd.articles@gmail.com2525-34092525-3409opendoar:2023-04-21T18:13:32Research, Society and Development - Universidade Federal de Itajubá (UNIFEI)false
dc.title.none.fl_str_mv Enhanced geranylgeraniol stability and dissolution from self-emulsifying pellets containing the sucupira (Pterodon emarginatus Vogel) standardized extract
Dissolución e estabilidad mejoradas de geranilgeraniol en péletes autoemulsionantes que contienen el extracto estandarizado de sucupira (Pterodon emarginatus Vogel)
Dissolução e estabilidade aprimoradas do geranilgeraniol em pellets autoemulsionáveis contendo o extrato padronizado de sucupira (Pterodon emarginatus Vogel)
title Enhanced geranylgeraniol stability and dissolution from self-emulsifying pellets containing the sucupira (Pterodon emarginatus Vogel) standardized extract
spellingShingle Enhanced geranylgeraniol stability and dissolution from self-emulsifying pellets containing the sucupira (Pterodon emarginatus Vogel) standardized extract
Alves, Suzana Ferreira
Plantas medicinais
Bioprodutos
Tecnologia fitofarmacêutica
SEDDS.
Plantas medicinales
Bioproductos
Tecnología farmacéutica
SEDDS.
Bioproducts
Phytopharmaceutical technology
Medicinal plants
SEDDS.
title_short Enhanced geranylgeraniol stability and dissolution from self-emulsifying pellets containing the sucupira (Pterodon emarginatus Vogel) standardized extract
title_full Enhanced geranylgeraniol stability and dissolution from self-emulsifying pellets containing the sucupira (Pterodon emarginatus Vogel) standardized extract
title_fullStr Enhanced geranylgeraniol stability and dissolution from self-emulsifying pellets containing the sucupira (Pterodon emarginatus Vogel) standardized extract
title_full_unstemmed Enhanced geranylgeraniol stability and dissolution from self-emulsifying pellets containing the sucupira (Pterodon emarginatus Vogel) standardized extract
title_sort Enhanced geranylgeraniol stability and dissolution from self-emulsifying pellets containing the sucupira (Pterodon emarginatus Vogel) standardized extract
author Alves, Suzana Ferreira
author_facet Alves, Suzana Ferreira
Marreto, Ricardo Neves
Bara, Maria Teresa Freitas
author_role author
author2 Marreto, Ricardo Neves
Bara, Maria Teresa Freitas
author2_role author
author
dc.contributor.author.fl_str_mv Alves, Suzana Ferreira
Marreto, Ricardo Neves
Bara, Maria Teresa Freitas
dc.subject.por.fl_str_mv Plantas medicinais
Bioprodutos
Tecnologia fitofarmacêutica
SEDDS.
Plantas medicinales
Bioproductos
Tecnología farmacéutica
SEDDS.
Bioproducts
Phytopharmaceutical technology
Medicinal plants
SEDDS.
topic Plantas medicinais
Bioprodutos
Tecnologia fitofarmacêutica
SEDDS.
Plantas medicinales
Bioproductos
Tecnología farmacéutica
SEDDS.
Bioproducts
Phytopharmaceutical technology
Medicinal plants
SEDDS.
description The vegetal species sucupira (Pterodon emarginatus Vogel) presents some diterpenes that have anti-inflammatory activities. However, diterpenes are poorly water-soluble compounds. The development of Self-Emulsifying Drug Delivery Systems (SEDDS) allows for obtaining a solid dosage form that maximizes the release of P. emarginatus constituents in an aqueous medium. This work aimed to obtain and characterize pellets containing the SEDDS prepared from P. emarginatus extract using the extrusion-spheronization technique. Formulations PF1 to PF6 were tested. Then, self-emulsifying formulations were prepared (SES1 to SES5) based on the mixture of poloxamer 188 (Pluronic® F-68) and sorbitan triolate (Span®85) with P. emarginatus extract. Next, formulation PF6, containing microcrystalline cellulose: P. emargitus extract: aerosil®200: polyvinylpyrrolindone K-30 (50: 54.25: 4: 4) was used in the preparation of pellets containing the self-emulsifying systems. These pellets had a homogeneous surface and average sphericity of 0.52. When encapsulated in hard gelatin capsules, it was noted that the formulations PF6, PSES3 and PSES4 were statistically different from each other at the 5% level. In the first 10 min of dissolution, PSES3 and PSES4 showed a higher level of geranylgeraniol released compared to the PF6 (p=0.000117). However, after 20 min of dissolution, no significant difference was observed in relation to the content of this compound. In the accelerated stability study, the average content of the geranylgeraniol was 85.6% and 81.8% for PSES3 and PSES4, respectively, whereas it was only 34.4% for PF6. Under the studied conditions, obtaining the self-emulsifying systems made it possible to achieve the desired dissolution and chemical stability of geranylgeraniol.
publishDate 2023
dc.date.none.fl_str_mv 2023-04-18
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv https://rsdjournal.org/index.php/rsd/article/view/41314
10.33448/rsd-v12i4.41314
url https://rsdjournal.org/index.php/rsd/article/view/41314
identifier_str_mv 10.33448/rsd-v12i4.41314
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv https://rsdjournal.org/index.php/rsd/article/view/41314/33588
dc.rights.driver.fl_str_mv Copyright (c) 2023 Suzana Ferreira Alves; Ricardo Neves Marreto; Maria Teresa Freitas Bara
https://creativecommons.org/licenses/by/4.0
info:eu-repo/semantics/openAccess
rights_invalid_str_mv Copyright (c) 2023 Suzana Ferreira Alves; Ricardo Neves Marreto; Maria Teresa Freitas Bara
https://creativecommons.org/licenses/by/4.0
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Research, Society and Development
publisher.none.fl_str_mv Research, Society and Development
dc.source.none.fl_str_mv Research, Society and Development; Vol. 12 No. 4; e26012441314
Research, Society and Development; Vol. 12 Núm. 4; e26012441314
Research, Society and Development; v. 12 n. 4; e26012441314
2525-3409
reponame:Research, Society and Development
instname:Universidade Federal de Itajubá (UNIFEI)
instacron:UNIFEI
instname_str Universidade Federal de Itajubá (UNIFEI)
instacron_str UNIFEI
institution UNIFEI
reponame_str Research, Society and Development
collection Research, Society and Development
repository.name.fl_str_mv Research, Society and Development - Universidade Federal de Itajubá (UNIFEI)
repository.mail.fl_str_mv rsd.articles@gmail.com
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