Influence of the Freeze-Drying Process on the Physicochemical and Biological Properties of Pre-heated Amphotericin B Micellar Systems

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dc.contributor.authorSiqueira, Scheyla D. V. S.
dc.contributor.authorSilva-Filho, Miguel A.
dc.contributor.authorSilva, Christian A.
dc.contributor.authorAraujo, Ivonete B.
dc.contributor.authorSilva, Acarilia E.
dc.contributor.authorFernandes-Pedrosa, Matheus F.
dc.contributor.authorOliveira, Anselmo Gomes de [UNESP]
dc.contributor.authorEgito, E. Socrates T.
dc.contributor.institutionUniversidade Federal do Rio Grande do Norte (UFRN)
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionLab Sistemas Dispersos
dc.date.accessioned2014-12-03T13:11:43Z
dc.date.available2014-12-03T13:11:43Z
dc.date.issued2014-06-01
dc.description.abstractThe moderate heat treatment of amphotericin B (AmB) in its micellar form (M-AmB) results in superaggregates (H-AmB) that present a substantially lower toxicity and similar activity. The aim of this work was to evaluate the H-AmB behavior after a freeze-drying process. H-AmB and M-AmB micelles were evaluated before and after freeze-drying concerning their physicochemical and biological properties by spectrophotometry and activity/toxicity assay, respectively. Four concentrations of M-AmB and H-AmB were studied aiming to correlate their aggregation state and the respective biological behavior: 50 mg L-1, 5 mg L-1, 0.5 mg L-1, and 0.05 mg L-1. Then, potassium leakage and hemoglobin leakage from red blood cells were used to evaluate the acute and chronic toxicity, respectively. The efficacy of M-AmB and H-AmB formulations was assessed by potassium leakage from Candida albicans and by the broth microdilution method. After heating, in addition to an evident turbidity, a slight blueshift from 327 to 323 nm was also observed at the concentrations of 50 and 5 mg L-1 for H-AmB. Additionally, an increase in the absorbance at 323 nm at the concentration of 0.5 mg L-1 was detected. Concerning the toxicity, H-AmB caused significantly lower hemoglobin leakage than M-AmB. These results were observed for H-AmB before and after freeze-drying. However, there was no difference between H-AmB and M-AmB concerning their activity. Accordingly, the freeze-drying cycle did not show any influence on the behavior of heated formulations, highlighting the suitability of such a method to produce a new AmB product with a long shelf life and with both greater efficiency and less toxicity.en
dc.description.affiliationUniv Fed Rio Grande Norte UFRN, Ctr Ciencias Saude CCS, Lab Sistemas Dispersos LASID, Programa Posgrad Ciencias Saude, Natal, RN, Brazil
dc.description.affiliationUniv Fed Rio Grande do Norte, LASID, CCS, Dept Farm, Natal, RN, Brazil
dc.description.affiliationUniv Fed Rio Grande do Norte, CCS, Dept Farm, Lab Tecnol & Biotecnol Farmaceut TecBioFar, Natal, RN, Brazil
dc.description.affiliationFac Ciencias Farmaceut UNESP, Dept Farmacos Med, BR-14801902 Araraquara, SP, Brazil
dc.description.affiliationLab Sistemas Dispersos, BR-59094450 Natal, RN, Brazil
dc.description.affiliationUnespFac Ciencias Farmaceut UNESP, Dept Farmacos Med, BR-14801902 Araraquara, SP, Brazil
dc.description.sponsorshipCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.format.extent612-619
dc.identifierhttp://dx.doi.org/10.1208/s12249-014-0085-z
dc.identifier.citationAaps Pharmscitech. New York: Springer, v. 15, n. 3, p. 612-619, 2014.
dc.identifier.doi10.1208/s12249-014-0085-z
dc.identifier.issn1530-9932
dc.identifier.lattes9114495952533044
dc.identifier.urihttp://hdl.handle.net/11449/113466
dc.identifier.wosWOS:000336729800010
dc.language.isoeng
dc.publisherSpringer
dc.relation.ispartofAaps Pharmscitech
dc.relation.ispartofjcr2.666
dc.relation.ispartofsjr0,752
dc.rights.accessRightsAcesso restrito
dc.sourceWeb of Science
dc.subjectactivityen
dc.subjectamphotericin Ben
dc.subjectfreeze-dryingen
dc.subjectheatingen
dc.subjecttoxicityen
dc.titleInfluence of the Freeze-Drying Process on the Physicochemical and Biological Properties of Pre-heated Amphotericin B Micellar Systemsen
dc.typeArtigo
dcterms.licensehttp://www.springer.com/open+access/authors+rights?SGWID=0-176704-12-683201-0
dcterms.rightsHolderSpringer
unesp.author.lattes9114495952533044[7]
unesp.author.orcid0000-0002-0107-9940[7]
unesp.author.orcid0000-0002-9889-6794[1]
unesp.author.orcid0000-0002-9997-4870[2]
unesp.author.orcid0000-0002-2180-3991[8]
unesp.author.orcid0000-0003-4221-9580[6]
unesp.campusUniversidade Estadual Paulista (Unesp), Faculdade de Ciências Farmacêuticas, Araraquarapt

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