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J Liposome Res ; 29(3): 264-273, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30501444

RESUMO

The purpose of this research was to develop cubosomal mucoadhesive in situ nasal gel to enhance the donepezil HCl delivery to the brain. Glycerol mono-oleate (GMO) and surfactant poloxamer 407 were used to prepare cubosomes. The developed formulations were characterized for particle size (PS), poly dispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE), transmission electron microscopy (TEM), in vitro drug release and in vivo bio-distribution study in blood and brain tissue. Central composite design was used for the optimization purpose and the selected formulation (containing GMO 2 g and poloxamer 1.5%) was prepared in presence of gellan gum and konjac gum as gelling agent and mucoadhesive agent respectively. The optimal cubosomal dispersion and optimal cubosomal mucoadhesive in situ nasal gel were subjected to in vivo bio-distribution studies in rat model. It showed significantly higher transnasal permeation and better distribution to the brain, when compared to the drug solution. Thus, the formulated cubosomal mucoadhesive in situ gel could be considered as a promising carrier for brain targeting of CNS acting drugs through the transnasal route.


Assuntos
Encéfalo/metabolismo , Donepezila/química , Lipossomos/química , Nanocápsulas/química , Animais , Preparações de Ação Retardada , Donepezila/farmacocinética , Liberação Controlada de Fármacos , Géis , Glicerídeos/química , Concentração de Íons de Hidrogênio , Masculino , Mucosa Nasal/metabolismo , Tamanho da Partícula , Poloxâmero/química , Ratos Sprague-Dawley , Distribuição Tecidual , Viscosidade
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