Preparation of polymeric micelles for use as carriers of tuberculostatic drugs

Página do item simplificado
dc.contributor.authorSilva, Marcia [UNESP]
dc.contributor.authorFerreira, Eiizabeth I.
dc.contributor.authorLeite, Clarice Queico Fujimura [UNESP]
dc.contributor.authorSato, Daisy N.
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionUniversidade de São Paulo (USP)
dc.contributor.institutionInstituto Adolfo Lutz (IAL)
dc.date.accessioned2014-05-20T13:24:31Z
dc.date.available2014-05-20T13:24:31Z
dc.date.issued2007-12-01
dc.description.abstractPurpose: This paper focuses on the characterization of polymeric micelle-forming tuberculostatic prodrugs and the antimycobacterial activity of these prodrugs.Method: By the condensation of hydroxymethylpyrazinamide, isoniazid and rifampin with free carboxyl groups on the copolymer poly(ethyleneglycol)-poly(aspartic acid), micelle-forming carrier-drug conjugates were obtained. These micelles were characterized by dynamic light scattering, to measure the micelle diameter; by acid-base titration, to determine the percentage of carboxylic groups occupied by the tuberculostatic; by Sudan III solubility tests, to estimate the critical micelle concentration (CMC); and visual control and spectrophotometric measurement, to determine the stability of micelles. These micelles were tested in vitro against several Mycobacterium strains.Results: As expected, the size and distribution of the micelle-forming tuberculostatic prodrugs found to be small (78.2nm, 84.2nm and 98.9 nm) while the level of the drug conjugated was high (65.02-85.7%). Furthermore, the micelles were stable in vitro, exhibiting a low level of CMC and stronger antimycobacterial activity than the original drugs.Conclusion: the results demonstrate that polymeric micelles can be used as efficient carriers for drugs, which alone, exhibit undesired pharmacokinetics, poor solubility, and low stability. The synthesized micelle-forming tuberculostatic prodrugs opens a perspective of alternative prodrugs that prolong action and decrease the toxicity of the tuberculostatic drugs of choice.en
dc.description.affiliationUNESP, Fac Ciências Farmaceut, Dept Farm & Med, Araraquara, SP, Brazil
dc.description.affiliationUniv São Paulo, Fac Ciências Farmaceut, Dept Farm, BR-09500900 São Paulo, Brazil
dc.description.affiliationUNESP, Fac Ciências Farmaceut, Dept Ciências Biol, Araraquara, SP, Brazil
dc.description.affiliationInst Adolfo Lutz Registro, Ribeirao Preto, Brazil
dc.description.affiliationUnespUNESP, Fac Ciências Farmaceut, Dept Farm & Med, Araraquara, SP, Brazil
dc.description.affiliationUnespUNESP, Fac Ciências Farmaceut, Dept Ciências Biol, Araraquara, SP, Brazil
dc.format.extent815-824
dc.identifierhttp://dx.doi.org/10.4314%2Ftjpr.v6i4.14665
dc.identifier.citationTropical Journal of Pharmaceutical Research. Benin City: Pharmacotherapy Group, v. 6, n. 4, p. 815-824, 2007.
dc.identifier.doi10.4314%2Ftjpr.v6i4.14665
dc.identifier.fileWOS000253261500004.pdf
dc.identifier.issn1596-5996
dc.identifier.lattes2114570774349859
dc.identifier.urihttp://hdl.handle.net/11449/7634
dc.identifier.wosWOS:000253261500004
dc.language.isoeng
dc.publisherPharmacotherapy Group
dc.relation.ispartofTropical Journal of Pharmaceutical Research
dc.relation.ispartofjcr0.444
dc.relation.ispartofsjr0,256
dc.rights.accessRightsAcesso aberto
dc.sourceWeb of Science
dc.subjectpyrazinamidept
dc.subjectisoniazidpt
dc.subjectrifampinpt
dc.subjecttuberculostatic prodrugspt
dc.subjectpolymer micellespt
dc.titlePreparation of polymeric micelles for use as carriers of tuberculostatic drugsen
dc.typeArtigo
dcterms.licensehttp://www.ajol.info/index.php/ajol/pages/view/TermsAndCond
dcterms.rightsHolderPharmacotherapy Group
unesp.author.lattes2114570774349859
unesp.campusUniversidade Estadual Paulista (Unesp), Faculdade de Ciências Farmacêuticas, Araraquarapt

Arquivos

Pacote Original
Agora exibindo 1 - 1 de 1
Imagem de Miniatura
Nome:
WOS000253261500004.pdf
Tamanho:
221.14 KB
Formato:
Adobe Portable Document Format
Baixar
Licença do Pacote
Agora exibindo 1 - 1 de 1
Nenhuma Miniatura disponível
Nome:
license.txt
Tamanho:
1.71 KB
Formato:
Item-specific license agreed upon to submission
Descrição:

Coleções

Artigos - Ciências Biológicas - FCFAR