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J Pharm Sci ; 108(9): 3082-3090, 2019 09.
Artículo en Inglés | MEDLINE | ID: mdl-31077685

RESUMEN

Intranasal nanostructured lipid carrier (NLC) of lurasidone hydrochloride (LRD) for brain delivery was prepared by the solvent evaporation method. The effects of independent variables, X1-lipid concentration, X-2 surfactant, and X-3 sonication times on dependent variables, Y1-particle size, Y-2 polydispersity index, and Y-3% entrapment efficiency were determined using Box-Behnken design. Optimized LRD-NLC was selected from the Box-Behnken design and evaluated for their morphological, physiological, nasal diffusion, and in vivo distribution in the brain after intranasal administration. Particle size, polydispersity index, and entrapment efficiency of optimized LRD-NLC were found to be 207.4 ± 1.5 nm, 0.392 ± 0.15, and 92.12 ± 1.0%, respectively. Transmission electron microscopy and scanning electron microscopy was used to determine the particle size and surface morphology of LRD-NLC. The prepared LRD-NLC follows biphasic in vitro drug release. Prepared NLC showed a 2-fold increase in LRD concentration in the brain when compared with the drug solution following intranasal administration. Results showed that intranasal route can be a good and efficient approach for delivering the drug directly to the brain and enhancing the drug efficacy in the brain for the management of schizophrenia and a good alternative to oral drug delivery.


Asunto(s)
Antipsicóticos/farmacocinética , Encéfalo/metabolismo , Portadores de Fármacos/química , Lípidos/química , Clorhidrato de Lurasidona/farmacocinética , Nanopartículas/química , Administración Intranasal , Animales , Antipsicóticos/administración & dosificación , Química Farmacéutica , Diseño de Fármacos , Humanos , Clorhidrato de Lurasidona/administración & dosificación , Masculino , Microscopía Electrónica de Rastreo , Microscopía Electrónica de Transmisión , Modelos Químicos , Nanopartículas/ultraestructura , Tamaño de la Partícula , Ratas , Ratas Wistar , Esquizofrenia/tratamiento farmacológico , Solubilidad , Propiedades de Superficie
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