Assessment of in vitro methodologies to determine topical and transdermal delivery of the flavonoid quercetin

To be effective against the oxidative damages induced by UVB irradiation in the skin, the drug needs to release from the formulation in which it was incorporated and reach the skin layers where the ROS are generated. Thus, it is very important the development of a robust and sensitive methodology to...

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Main Authors: Fabiana Testa Moura de Carvalho Vicentini, Sandra Regina Georgetti, Maria Vitória Lopes Badra Bentley, Maria José Vieira Fonseca
Format: Article
Language:English
Published: Universidade de São Paulo 2009-06-01
Series:Brazilian Journal of Pharmaceutical Sciences
Subjects:
Online Access:http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502009000200022
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author Fabiana Testa Moura de Carvalho Vicentini
Sandra Regina Georgetti
Maria Vitória Lopes Badra Bentley
Maria José Vieira Fonseca
author_facet Fabiana Testa Moura de Carvalho Vicentini
Sandra Regina Georgetti
Maria Vitória Lopes Badra Bentley
Maria José Vieira Fonseca
author_sort Fabiana Testa Moura de Carvalho Vicentini
collection DOAJ
description To be effective against the oxidative damages induced by UVB irradiation in the skin, the drug needs to release from the formulation in which it was incorporated and reach the skin layers where the ROS are generated. Thus, it is very important the development of a robust and sensitive methodology to extract and quantify in different skin layers the antioxidant agent delivered from topical formulations. Therefore, in the present work suitable methods to extract and quantify quercetin in skin samples and receptor phase after in vitro penetration studies were developed. The results demonstrated that the recovery from two different layers of skin, the SC and [E+D], using two different methods of quantification (DPPH• assay and HPLC, respectively), was 93.8 % when the quercetin spiked dose was 50 µg/mL, 100.4 % when it was 100 µg/mL and 89.9 % for 250 µg/mL and the average recovery of the quercetin extraction from receptor phase when dichloromethane was used as extractor solvent was 96%. These results demonstrate that the described methods have a potential application to in vitro skin penetration studies of quercetin, since it showed to be accurate and sensitive.<br>Para ser efetiva contra os danos oxidativos induzidos pela radiação UVB na pele, é necessário que o ativo seja liberado da formulação na qual foi incorporado e alcance as camadas da pele onde são geradas as EROS. Desta forma, torna-se de grande importância o desenvolvimento de métodos eficazes e sensíveis para extrair e quantificar, nas diferentes camadas de pele, o agente antioxidante liberado de formulações tópicas. No presente trabalho foram desenvolvidos métodos adequados para extrair e quantificar a quercetina em amostras de pele e na fase receptora após estudos de penetração cutânea in vitro. Os resultados demonstraram que a recuperação das camadas de pele, EC e [E+D], quando do uso de duas diferentes metodologias de quantificação (ensaio de DPPH• e CLAE, respectivamente), foi de 93,8 % quando aplicada uma dose de 50 µg/mL de quercetina, 100,4 % para 100 µg/mL e 89,9 % para 250 µg/mL e a recuperação média da extração da quercetina da fase receptora, quando do emprego de diclorometano como solvente extrator, foi de 96 %. Tais resultados demonstram que os métodos descritos têm grande potencial de aplicação em estudos de penetração in vitro já que apresentaram exatidão e sensibilidade.
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spelling doaj.art-2d0c14774d6e4b92998fc407ffcd36342022-12-22T02:49:30ZengUniversidade de São PauloBrazilian Journal of Pharmaceutical Sciences1984-82502175-97902009-06-0145235736410.1590/S1984-82502009000200022Assessment of in vitro methodologies to determine topical and transdermal delivery of the flavonoid quercetinFabiana Testa Moura de Carvalho VicentiniSandra Regina GeorgettiMaria Vitória Lopes Badra BentleyMaria José Vieira FonsecaTo be effective against the oxidative damages induced by UVB irradiation in the skin, the drug needs to release from the formulation in which it was incorporated and reach the skin layers where the ROS are generated. Thus, it is very important the development of a robust and sensitive methodology to extract and quantify in different skin layers the antioxidant agent delivered from topical formulations. Therefore, in the present work suitable methods to extract and quantify quercetin in skin samples and receptor phase after in vitro penetration studies were developed. The results demonstrated that the recovery from two different layers of skin, the SC and [E+D], using two different methods of quantification (DPPH• assay and HPLC, respectively), was 93.8 % when the quercetin spiked dose was 50 µg/mL, 100.4 % when it was 100 µg/mL and 89.9 % for 250 µg/mL and the average recovery of the quercetin extraction from receptor phase when dichloromethane was used as extractor solvent was 96%. These results demonstrate that the described methods have a potential application to in vitro skin penetration studies of quercetin, since it showed to be accurate and sensitive.<br>Para ser efetiva contra os danos oxidativos induzidos pela radiação UVB na pele, é necessário que o ativo seja liberado da formulação na qual foi incorporado e alcance as camadas da pele onde são geradas as EROS. Desta forma, torna-se de grande importância o desenvolvimento de métodos eficazes e sensíveis para extrair e quantificar, nas diferentes camadas de pele, o agente antioxidante liberado de formulações tópicas. No presente trabalho foram desenvolvidos métodos adequados para extrair e quantificar a quercetina em amostras de pele e na fase receptora após estudos de penetração cutânea in vitro. Os resultados demonstraram que a recuperação das camadas de pele, EC e [E+D], quando do uso de duas diferentes metodologias de quantificação (ensaio de DPPH• e CLAE, respectivamente), foi de 93,8 % quando aplicada uma dose de 50 µg/mL de quercetina, 100,4 % para 100 µg/mL e 89,9 % para 250 µg/mL e a recuperação média da extração da quercetina da fase receptora, quando do emprego de diclorometano como solvente extrator, foi de 96 %. Tais resultados demonstram que os métodos descritos têm grande potencial de aplicação em estudos de penetração in vitro já que apresentaram exatidão e sensibilidade.http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502009000200022Formulações tópicasQuercetinaQuercetinaQuercetinaPenetração cutânea in vitroCromatografia líquida de alta eficiênciaDPPH•Topical formulationsQuercetinQuercetinQuercetinSkin penetration in vitroHigh performance liquid chromatographyDPPH•
spellingShingle Fabiana Testa Moura de Carvalho Vicentini
Sandra Regina Georgetti
Maria Vitória Lopes Badra Bentley
Maria José Vieira Fonseca
Assessment of in vitro methodologies to determine topical and transdermal delivery of the flavonoid quercetin
Brazilian Journal of Pharmaceutical Sciences
Formulações tópicas
Quercetina
Quercetina
Quercetina
Penetração cutânea in vitro
Cromatografia líquida de alta eficiência
DPPH•
Topical formulations
Quercetin
Quercetin
Quercetin
Skin penetration in vitro
High performance liquid chromatography
DPPH•
title Assessment of in vitro methodologies to determine topical and transdermal delivery of the flavonoid quercetin
title_full Assessment of in vitro methodologies to determine topical and transdermal delivery of the flavonoid quercetin
title_fullStr Assessment of in vitro methodologies to determine topical and transdermal delivery of the flavonoid quercetin
title_full_unstemmed Assessment of in vitro methodologies to determine topical and transdermal delivery of the flavonoid quercetin
title_short Assessment of in vitro methodologies to determine topical and transdermal delivery of the flavonoid quercetin
title_sort assessment of in vitro methodologies to determine topical and transdermal delivery of the flavonoid quercetin
topic Formulações tópicas
Quercetina
Quercetina
Quercetina
Penetração cutânea in vitro
Cromatografia líquida de alta eficiência
DPPH•
Topical formulations
Quercetin
Quercetin
Quercetin
Skin penetration in vitro
High performance liquid chromatography
DPPH•
url http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502009000200022
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