Development and characterization of a new oral dapsone nanoemulsion system: permeability and in silico bioavailability studies

Development and characterization of a new oral dapsone nanoemulsion system: permeability and in silico bioavailability studies

Lidiane M Monteiro,1 Viviane F Lione,1 Flavia A do Carmo,1 Lilian H do Amaral,1 Julianna H da Silva,2 Luiz E Nasciutti,2 Carlos R Rodrigues,1 Helena C Castro,3 Valeria P de Sousa,1 Lucio M Cabral11Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, 2Instituto de Ci&...

Descripción completa

Guardado en:
Detalles Bibliográficos
Autores principales: Monteiro LM, Lione VF, do Carmo FA, do Amaral LH, da Silva JH, Nasciutti LE, Rodrigues CR, Castro HC, de Sousa VP, Cabral LM
Formato: article
Lenguaje:EN
Publicado: Dove Medical Press 2012
Materias:
Medicine (General)
R5-920
Acceso en línea:https://doaj.org/article/7b61031b87894e1096f56763a7ffd770
Etiquetas: Agregar Etiqueta
Sin Etiquetas, Sea el primero en etiquetar este registro!
id oai:doaj.org-article:7b61031b87894e1096f56763a7ffd770
record_format dspace
spelling oai:doaj.org-article:7b61031b87894e1096f56763a7ffd7702021-12-02T02:16:49ZDevelopment and characterization of a new oral dapsone nanoemulsion system: permeability and in silico bioavailability studies1176-91141178-2013https://doaj.org/article/7b61031b87894e1096f56763a7ffd7702012-09-01T00:00:00Zhttp://www.dovepress.com/development-and-characterization-of-a-new-oral-dapsone-nanoemulsion-sy-a11141https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Lidiane M Monteiro,1 Viviane F Lione,1 Flavia A do Carmo,1 Lilian H do Amaral,1 Julianna H da Silva,2 Luiz E Nasciutti,2 Carlos R Rodrigues,1 Helena C Castro,3 Valeria P de Sousa,1 Lucio M Cabral11Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, 2Instituto de Ciências Biomédicas, Universidade Federal do Rio de Janeiro, 3Instituto de Biologia, Universidade Federal Fluminense, Niterói, Rio de Janeiro, BrasilBackground: Dapsone is described as being active against Mycobacterium leprae, hence its role in the treatment of leprosy and related pathologies. Despite its therapeutic potential, the low solubility of dapsone in water results in low bioavailability and high microbial resistance. Nanoemulsions are pharmaceutical delivery systems derived from micellar solutions with a good capacity for improving absorption. The aim of this work was to develop and compare the permeability of a series of dapsone nanoemulsions in Caco-2 cell culture against that of effective permeability in the human body simulated using GastroplusTM software.Methods and results: The release profiles of the dapsone nanoemulsions using different combinations of surfactants and cosolvent showed a higher dissolution rate in simulated gastric and enteric fluid than did the dispersed dapsone powder. The drug release kinetics were consistent with a Higuchi model.Conclusion: This comparison of dapsone permeability in Caco-2 cells with effective permeability in the human body simulated by Gastroplus showed a good correlation and indicates potential improvement in the biodisponibility of dapsone using this new system.Keywords: dapsone, nanoemulsions, antibacterial, permeability, Caco-2 cell, GastroplusTMMonteiro LMLione VFdo Carmo FAdo Amaral LHda Silva JHNasciutti LERodrigues CRCastro HCde Sousa VPCabral LMDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 5175-5182 (2012)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Monteiro LM
Lione VF
do Carmo FA
do Amaral LH
da Silva JH
Nasciutti LE
Rodrigues CR
Castro HC
de Sousa VP
Cabral LM
Development and characterization of a new oral dapsone nanoemulsion system: permeability and in silico bioavailability studies
description Lidiane M Monteiro,1 Viviane F Lione,1 Flavia A do Carmo,1 Lilian H do Amaral,1 Julianna H da Silva,2 Luiz E Nasciutti,2 Carlos R Rodrigues,1 Helena C Castro,3 Valeria P de Sousa,1 Lucio M Cabral11Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, 2Instituto de Ciências Biomédicas, Universidade Federal do Rio de Janeiro, 3Instituto de Biologia, Universidade Federal Fluminense, Niterói, Rio de Janeiro, BrasilBackground: Dapsone is described as being active against Mycobacterium leprae, hence its role in the treatment of leprosy and related pathologies. Despite its therapeutic potential, the low solubility of dapsone in water results in low bioavailability and high microbial resistance. Nanoemulsions are pharmaceutical delivery systems derived from micellar solutions with a good capacity for improving absorption. The aim of this work was to develop and compare the permeability of a series of dapsone nanoemulsions in Caco-2 cell culture against that of effective permeability in the human body simulated using GastroplusTM software.Methods and results: The release profiles of the dapsone nanoemulsions using different combinations of surfactants and cosolvent showed a higher dissolution rate in simulated gastric and enteric fluid than did the dispersed dapsone powder. The drug release kinetics were consistent with a Higuchi model.Conclusion: This comparison of dapsone permeability in Caco-2 cells with effective permeability in the human body simulated by Gastroplus showed a good correlation and indicates potential improvement in the biodisponibility of dapsone using this new system.Keywords: dapsone, nanoemulsions, antibacterial, permeability, Caco-2 cell, GastroplusTM
format article
author Monteiro LM
Lione VF
do Carmo FA
do Amaral LH
da Silva JH
Nasciutti LE
Rodrigues CR
Castro HC
de Sousa VP
Cabral LM
author_facet Monteiro LM
Lione VF
do Carmo FA
do Amaral LH
da Silva JH
Nasciutti LE
Rodrigues CR
Castro HC
de Sousa VP
Cabral LM
author_sort Monteiro LM
title Development and characterization of a new oral dapsone nanoemulsion system: permeability and in silico bioavailability studies
title_short Development and characterization of a new oral dapsone nanoemulsion system: permeability and in silico bioavailability studies
title_full Development and characterization of a new oral dapsone nanoemulsion system: permeability and in silico bioavailability studies
title_fullStr Development and characterization of a new oral dapsone nanoemulsion system: permeability and in silico bioavailability studies
title_full_unstemmed Development and characterization of a new oral dapsone nanoemulsion system: permeability and in silico bioavailability studies
title_sort development and characterization of a new oral dapsone nanoemulsion system: permeability and in silico bioavailability studies
publisher Dove Medical Press
publishDate 2012
url https://doaj.org/article/7b61031b87894e1096f56763a7ffd770
work_keys_str_mv AT monteirolm developmentandcharacterizationofaneworaldapsonenanoemulsionsystempermeabilityandinsilicobioavailabilitystudies
AT lionevf developmentandcharacterizationofaneworaldapsonenanoemulsionsystempermeabilityandinsilicobioavailabilitystudies
AT docarmofa developmentandcharacterizationofaneworaldapsonenanoemulsionsystempermeabilityandinsilicobioavailabilitystudies
AT doamarallh developmentandcharacterizationofaneworaldapsonenanoemulsionsystempermeabilityandinsilicobioavailabilitystudies
AT dasilvajh developmentandcharacterizationofaneworaldapsonenanoemulsionsystempermeabilityandinsilicobioavailabilitystudies
AT nasciuttile developmentandcharacterizationofaneworaldapsonenanoemulsionsystempermeabilityandinsilicobioavailabilitystudies
AT rodriguescr developmentandcharacterizationofaneworaldapsonenanoemulsionsystempermeabilityandinsilicobioavailabilitystudies
AT castrohc developmentandcharacterizationofaneworaldapsonenanoemulsionsystempermeabilityandinsilicobioavailabilitystudies
AT desousavp developmentandcharacterizationofaneworaldapsonenanoemulsionsystempermeabilityandinsilicobioavailabilitystudies
AT cabrallm developmentandcharacterizationofaneworaldapsonenanoemulsionsystempermeabilityandinsilicobioavailabilitystudies
_version_ 1718402604372852736

Ejemplares similares