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dc.contributor.authorCatalán-Figueroa, Johanna [Univ Mayor, Ctr Nanotecnol Aplicada, Santiago, Chile]es_CL
dc.contributor.authorFiedler, Jenny L. [Univ Mayor, Ctr Nanotecnol Aplicada, Santiago, Chile]es_CL
dc.contributor.authorBoisset, Constanza B.es_CL
dc.contributor.authorJara, Miguel O.es_CL
dc.contributor.authorFlores, Mario E.es_CL
dc.contributor.authorMoreno-Villoslada, Ignacioes_CL
dc.contributor.authorMorales, Javier O.es_CL
dc.date.accessioned2020-04-08T14:11:55Z
dc.date.accessioned2020-04-13T18:12:51Z
dc.date.available2020-04-08T14:11:55Z
dc.date.available2020-04-13T18:12:51Z
dc.date.issued2018es_CL
dc.identifier.citationCatalan-Figueroa, J., Boisset, C. B., Jara, M. O., Flores, M. E., Moreno-Villoslada, I., Fiedler, J. L., & Morales, J. O. (2018). A mechanistic approach for the optimization of loperamide loaded nanocarriers characterization: Diafiltration and mathematical modeling advantages. European Journal of Pharmaceutical Sciences, 125, 215-222.es_CL
dc.identifier.issn0928-0987es_CL
dc.identifier.issn1879-0720es_CL
dc.identifier.urihttps://doi.org/10.1016/j.ejps.2018.10.002es_CL
dc.identifier.urihttp://repositorio.umayor.cl/xmlui/handle/sibum/6261
dc.description.abstractOral bioavailability of loperamide is restricted by its limited absorption in the gastrointestinal tract due to its poor aqueous solubility and its P-glycoprotein (Pgp) substrate characteristic. In addition, ammonium methacrylate copolymers have shown to have mucoadhesive properties, whereas poloxamer 188, has been suggested as a Pgp inhibitor. Thus, in this work, we evaluate conditions that affect physicochemical parameters of ammonium methacrylate/poloxamer 188-based nanocarriers loaded with loperamide hydrochloride. Nanocarriers were synthesized by nanoprecipitation, enhancing loperamide encapsulation efficiency by modifying the aqueous phase to basic pH. The isolation of the non-encapsulated drug fraction from the nanocarriers-incorporated fraction was conducted by centrifugation, ultrafiltration, vacuum filtration and diafiltration. The last method was effective in providing a deeper understanding of drug-nanocarrier loading and interactions by means of modeling the data obtained by it. Through diafiltration, it was determined an encapsulation efficiency of about 93%, from which a 38% +/- 6 was shown to be reversibly (thermodynamic interaction) and a 62% +/- 6 irreversibly (kinetic interaction) bound. Finally, release profiles were assessed through empirical and semi-empirical modeling, showing a biphasic release behavior (burst effect 11.34% and total release at 6 h = 33% +/- 1). Thus, encapsulation efficiency and release profile were shown to have a strong mathematical modeling-based correlation, providing the mechanistic approach presented in this article a solid support for future translational investigations.es_CL
dc.description.sponsorshipFONDECYTComision Nacional de Investigacion Cientifica y Tecnologica (CONICYT)CONICYT FONDECYT [1150899, 1181689]; FONDAP [15130011]; CONICYTComision Nacional de Investigacion Cientifica y Tecnologica (CONICYT) [21120192]es_CL
dc.description.sponsorshipThis work was supported by FONDECYT Regular 1150899 and 1181689, FONDAP 15130011, and CONICYT 21120192.es_CL
dc.language.isoenes_CL
dc.publisherELSEVIER SCIENCE BVes_CL
dc.rightsAttribution-NonCommercial-NoDerivs 3.0 Chile
dc.sourceEur. J. Pharm. Sci., DIC 2018. 125: p. 215-222
dc.subjectPharmacology & Pharmacyes_CL
dc.titleA mechanistic approach for the optimization of loperamide loaded nanocarriers characterization: Diafiltration and mathematical modeling advantageses_CL
dc.typeArtículoes_CL
umayor.facultadCIENCIASes_CL
umayor.politicas.sherpa/romeoRoMEO green journal (Se puede archivar el pre-print y el post-print o versión de editor/PDF). Disponible en: http://sherpa.ac.uk/romeo/index.phpes_CL
umayor.indexadoWOS:000448169800022es_CL
umayor.indexadoPMID: 30312746es_CL
dc.identifier.doiDOI: 10.1016/j.ejps.2018.10.002es_CL]
umayor.indicadores.wos-(cuartil)Q2es_CL
umayor.indicadores.scopus-(scimago-sjr)SCIMAGO/ INDICE H: 119 Hes_CL


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