Preparation of polymeric micelles for use as carriers of tuberculostatic drugs

dc.contributorUniversidade Estadual Paulista (UNESP)
dc.creatorSilva, Marcia
dc.creatorFerreira, Eiizabeth I.
dc.creatorLeite, Clarice Queico Fujimura
dc.creatorSato, Daisy N.
dc.date2014-05-20T13:24:31Z
dc.date2014-05-20T13:24:31Z
dc.date2007-12-01
dc.date.accessioned2017-04-05T20:00:30Z
dc.date.available2017-04-05T20:00:30Z
dc.identifierTropical Journal of Pharmaceutical Research. Benin City: Pharmacotherapy Group, v. 6, n. 4, p. 815-824, 2007.
dc.identifier1596-5996
dc.identifierhttp://hdl.handle.net/11449/7634
dc.identifier10.4314%2Ftjpr.v6i4.14665
dc.identifierWOS:000253261500004
dc.identifierWOS000253261500004.pdf
dc.identifierhttp://dx.doi.org/10.4314%2Ftjpr.v6i4.14665
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/856231
dc.descriptionPurpose: 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.
dc.languageeng
dc.publisherPharmacotherapy Group
dc.relationTropical Journal of Pharmaceutical Research
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectpyrazinamide
dc.subjectisoniazid
dc.subjectrifampin
dc.subjecttuberculostatic prodrugs
dc.subjectpolymer micelles
dc.titlePreparation of polymeric micelles for use as carriers of tuberculostatic drugs
dc.typeOtro


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