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dc.contributor.author
Leonardi, Darío
dc.contributor.author
Bombardiere, Maria Eugenia
dc.contributor.author
Salomon, Claudio Javier
dc.date.available
2016-06-02T18:50:20Z
dc.date.issued
2013-10
dc.identifier.citation
Leonardi, Darío; Bombardiere, Maria Eugenia; Salomon, Claudio Javier; Effects of benznidazole:cyclodextrin complexes on the drugbioavailability upon oral administration to rats; Elsevier; International Journal of Biological Macromolecules; 62; 10-2013; 543-548
dc.identifier.issn
0141-8130
dc.identifier.uri
http://hdl.handle.net/11336/6021
dc.description.abstract
Benznidazole (BZL) is the drug of choice for the treatment of Chagas´ s disease, a neglected parasitic infection. It is poorly soluble in water, which may have a direct impact into its bioavailability. Thus, the aim of this study was to evaluate the impact of stoichiometric and non-stoichiometric BZL:cyclodextrins (CDs) complexes on the bioavailability of BZL. The interaction of BZL with the CDs was investigated using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray diffractometry (XRD), phase solubility and dissolution studies. The oral bioavailability of BZL from these complexes was examined in rats. Both BZL solubility and dissolution increased by CD complexation. The inclusion complexes were found to improve the dissolution rate of BZL by 4.3-fold in comparison with BZL alone. Complexation of BZL with CDs derivatives increased its plasma concentrations when fed to rats, with AUC values increasing up to 3.7-fold and increasing 2.5-fold in comparison with BZL alone. It should be note that a remarkable increase in these parameters was observed in the case of the non-stoichiometric complexes. Thus, these CDs complexes could be used to efficiently deliver BZL in patients suffering from Chagas´ s disease.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Elsevier
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
dc.subject
Chagas´ Disease
dc.subject
Complexation
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Cyclodextrins
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Dissolution Rate
dc.subject.classification
Otras Ciencias de la Salud
dc.subject.classification
Ciencias de la Salud
dc.subject.classification
CIENCIAS MÉDICAS Y DE LA SALUD
dc.title
Effects of benznidazole:cyclodextrin complexes on the drugbioavailability upon oral administration to rats
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2016-06-01T13:35:11Z
dc.journal.volume
62
dc.journal.pagination
543-548
dc.journal.pais
Países Bajos
dc.journal.ciudad
Amsterdam
dc.description.fil
Fil: Leonardi, Darío. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Rosario. Instituto de Química Rosario; Argentina
dc.description.fil
Fil: Bombardiere, Maria Eugenia. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Rosario. Instituto de Química Rosario; Argentina
dc.description.fil
Fil: Salomon, Claudio Javier. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas; Argentina
dc.journal.title
International Journal of Biological Macromolecules
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0141813013005515
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.ijbiomac.2013.10.007
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/10.1016/j.ijbiomac.2013.10.007
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