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Estudio de las propiedades fisicoquímicas y antimicóticas de complejos entre un polielectrolito y el ácido benzoico como molécula modelo

dc.contributor.advisorBaena Aristizábal, Yolimaspa
dc.contributor.advisorManzo, Rubén Hilariospa
dc.contributor.authorDallos Morantes, Leidy Johannaspa
dc.contributor.researchgroupSILICOMOBAspa
dc.date.accessioned2020-03-10T13:31:06Zspa
dc.date.available2020-03-10T13:31:06Zspa
dc.date.issued2019-03-15spa
dc.description.abstractLa interacción de polielectrolitos con contraiones de uso farmacéutico ha sido aprovechada con múltiples propósitos, tales como la modulación de liberación, aumento de estabilidad de activos e incluso como potenciador de actividad bactericida. Sin embargo, pocos son los reportes de complejación de polielectrolitos con compuestos antimicóticos o con excipientes. La presente investigación buscó obtener complejos polielectrolito (CPE), de diferente composición, entre el polímero catiónico Eudragit® E100 y el ácido benzoico (agente preservante) y, evaluar sus propiedades fisicoquímicas y antimicóticas, para establecer posibles correlaciones entre ellas. Los resultados demostraron la apropiada obtención, por el método de evaporación de solvente, de diez composiciones de CPE (diferentes en el porcentaje de grupos amino del policatión neutralizado con el contraión benzoato y/o cloruro). Todas las propiedades fisicoquímicas estudiadas: patrones de difracción de rayos X, temperatura de transición vítrea, solubilidad, constante de afinidad, desplazamiento de ácido benzoico por intercambio iónico, evaluación de la carga de superficie y el comportamiento de liberación, demostraron dependencia de la composición de los CPE. Los estudios de actividad realizados frente a los hongos: Candida albicans, Aspergillus brasiliensis y Penicillium rubens, por su parte, evidenciaron que, a condiciones de pH controlado, los complejos con mayor porcentaje de contraión benzoato contaban con un mayor efecto sobre los hongos filamentosos, mientras que, los resultados en la levadura fueron independientes de la composición. El polímero neutralizado únicamente con HCl, también exhibió actividad frente a los tres microorganismos. La correlación de las variables fisicoquímicas con las antimicóticas para A. brasiliensis y P. rubens demostró relación directa para solubilidad, pseudo-potencial z y liberación. La causalidad de las correlaciones fue asociada a la interacción entre la carga de los CPE con los hongos y a la cantidad de activo disponible para ingresar a la célula.spa
dc.description.abstractThe unique properties arising from the interaction of PE with inorganic or organic counterions have been explored for a variety of purposes such as drug delivery modulation, drug stability improvement and as bactericidal activity enhancer. However, there are few studies involving complexation between polyelectrolytes and antimycotic agents or excipients. The aim of the present study was focused on polyelectrolyte complex formation (PEC) between Eudragit® E100 (cationic polymer) and benzoic acid (preservative agent) obtaining a set of complexes with different composition. Physicochemical properties and antimycotic activity were evaluated in order to stablish possible correlation. Results demonstrated the complexes formation, using solvent evaporation method, out of ten different PEC compositions (difference lies in neutralization amino group percentage by benzoate/chloride as counterion). The following properties were studied: X-ray diffraction, thermal analysis, solubility, counterionic condensation constant, benzoate displacement by ion exchange, surface charge and release profile. Evaluation of these properties proved that results are depending on PEC composition. Regarding with antimycotic activity, fungi Candida albicans, Aspergillus brasiliensis and Penicillium rubens, showed that at fixed pH values, complexes with higher counterion benzoate percentage lead to higher activity on filamentous fungi whilst activity on yeast was independent of PEC composition. Polymer amino groups were also completely neutralized with hydrochloric acid and its antimycotic activity was evaluated and it exhibited activity on fungi. Physicochemical properties and antimycotic activity are directly correlated for A. brasiliensis and P. rubens concerning to solubility, pseudo z potencial and release profile. This relation might be explained by interaction of PEC charge with fungi and benzoate amount available to cross cell membrane.spa
dc.description.additionalDoctora en Ciencias Farmacéuticas. Línea de Investigación: Sistemas conformados por complejos con polielectrolitosspa
dc.description.degreelevelDoctoradospa
dc.format.extent255spa
dc.format.mimetypeapplication/pdfspa
dc.identifier.citationDallos Morantes, L.J. (2019). Estudio de las propiedades fisicoquímicas y antimicóticas de complejos entre un polielectrolito y el ácido benzoico como molécula modelo. (Doctorado). Universidad Nacional de Colombia.spa
dc.identifier.urihttps://repositorio.unal.edu.co/handle/unal/76037
dc.language.isospaspa
dc.publisher.branchUniversidad Nacional de Colombia - Sede Bogotáspa
dc.publisher.departmentDepartamento de Farmaciaspa
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dc.rightsDerechos reservados - Universidad Nacional de Colombiaspa
dc.rights.accessrightsinfo:eu-repo/semantics/openAccessspa
dc.rights.licenseAtribución-NoComercial 4.0 Internacionalspa
dc.rights.spaAcceso abiertospa
dc.rights.urihttp://creativecommons.org/licenses/by-nc/4.0/spa
dc.subject.ddcFarmacotécniaspa
dc.subject.ddcActividad antimicóticaspa
dc.subject.proposalPolielectrolitospa
dc.subject.proposalPolyelectrolyte complexeng
dc.subject.proposalComplejaciónspa
dc.subject.proposalBenzoic acideng
dc.subject.proposalÁcido benzoicospa
dc.subject.proposalEudragit® E100eng
dc.subject.proposalAntimycotic activityeng
dc.subject.proposalEudragit® E100spa
dc.subject.proposalActividad antimicóticaspa
dc.titleEstudio de las propiedades fisicoquímicas y antimicóticas de complejos entre un polielectrolito y el ácido benzoico como molécula modelospa
dc.title.alternativePhysicochemical and antimycotic properties of polyelectrolyte complexes with benzoic acid as model molecule.spa
dc.typeTrabajo de grado - Doctoradospa
dc.type.coarhttp://purl.org/coar/resource_type/c_db06spa
dc.type.coarversionhttp://purl.org/coar/version/c_ab4af688f83e57aaspa
dc.type.contentTextspa
dc.type.driverinfo:eu-repo/semantics/doctoralThesisspa
dc.type.versioninfo:eu-repo/semantics/acceptedVersionspa
oaire.accessrightshttp://purl.org/coar/access_right/c_abf2spa

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