Design of an innovative nanovehicle to enhance brain permeability of a novel 5-HT6 receptor antagonist

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dc.contributor.authorAlvarez-Figueroa, Maria Javiera
dc.contributor.authorNunez-Navarro, Francisco
dc.contributor.authorRecabarren-Gajardo, Gonzalo
dc.contributor.authorGonzalez-Aramundiz, Jose Vicente
dc.date.accessioned2025-01-20T16:04:36Z
dc.date.available2025-01-20T16:04:36Z
dc.date.issued2024
dc.description.abstractAn innovative nanovehicle based on lipid nanocapsules (LNC) was designed to facilitate the passage of a new 5HT6 receptor antagonist, namely PUC-10, through the blood-brain barrier. PUC-10 is a new synthetic N-arylsulfonylindole that has demonstrated potent 5-HT6 receptor antagonist activity, but it exhibits poor solubility in water, which indicates limited absorption. The lipid nanocapsules designed had a nanometric size (53 nm), a monomodal distribution (PI<0.2), a negative Z potential (-17 +/- 7 mV) and allowed efficient PUC-10 encapsulation (74 %). Furthermore, the LNC demonstrated to be stable for at least 4 weeks at 4( degrees)C (storage conditions), for at least 4 h in DMEM at pH 7.4, and for 18 h in water with 5 % DMSO, with both latter conditions maintained at 37 C-degrees. They also demonstrated that cell viability was not affected at the different concentrations studied. Finally, in vitro studies that simulate the blood brain barrier (PAMPA-BBB) demonstrated that the nanoencapsulation of PUC-10 promoted their penetration through the blood-brain barrier, with a calculated permeability of 1.3 x 10(- 8 )cm/s, compared to the null permeability exhibited by non-nanoencapsulated PUC-10.
dc.fuente.origenWOS
dc.identifier.doi10.1016/j.ijpx.2024.100296
dc.identifier.eissn2590-1567
dc.identifier.urihttps://doi.org/10.1016/j.ijpx.2024.100296
dc.identifier.urihttps://repositorio.uc.cl/handle/11534/89813
dc.identifier.wosidWOS:001349297000001
dc.language.isoen
dc.revistaInternational journal of pharmaceutics-x
dc.rightsacceso restringido
dc.subjectLipid nanocapsules
dc.subjectPAMPA-BBB
dc.subjectBrain permeability
dc.subjectArylsulfonylindoles
dc.subject5-HT6 receptor
dc.titleDesign of an innovative nanovehicle to enhance brain permeability of a novel 5-HT6 receptor antagonist
dc.typeartículo
dc.volumen8
sipa.indexWOS
sipa.trazabilidadWOS;2025-01-12
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