Cannabinoid antagonist in nanostructured lipid carriers (NLCs): design, characterization and in vivo study.
Mater Sci Eng C Mater Biol Appl
; 48: 328-36, 2015 Mar.
Article
em En
| MEDLINE
| ID: mdl-25579930
ABSTRACT
This study describes the preparation, characterization, and in vivo evaluation in rats of nanostructured lipid carriers (NLCs) encapsulating rimonabant (RMN) as prototypical cannabinoid antagonist. A study was conducted in order to optimize NLC production by melt and ultrasonication method. NLCs were prepared by alternatively adding the lipid phase into the aqueous one (direct protocol) or the aqueous phase into the lipid one (reverse protocol). RMN-NLCs have been characterized by cryogenic transmission electron microscopy (cryo-TEM), X-ray, photon correlation spectroscopy (PCS) and sedimentation field flow fractionation (SdFFF). Reverse NLCs were treated with polysorbate 80. RMN release kinetics have been determined in vitro by dialysis method. In vivo RMN biodistribution in rats was evaluated after intranasal (i.n.) administration of reverse RMN-NLC. The reverse protocol enabled to prevent the lost of lipid phase and to achieve higher RMN encapsulation efficacy (EE) with respect to the direct protocol (98% w/w versus 67% w/w). The use of different protocols did not affect NLC morphology and dimensional distribution. An in vitro dissolutive release rate of RMN was calculated. The in vivo data indicate that i.n. administration of RMN by reverse NLC treated with polysorbate 80 increased RMN concentration in the brain with respect to the drug in solution. The nanoencapsulation protocol presented here appears as an optimal strategy to improve the low solubility of cannabinoid compounds in an aqueous system suitable for in vivo administration.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piperidinas
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Pirazóis
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Nanocápsulas
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Antagonistas de Receptores de Canabinoides
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Lipídeos
Limite:
Animals
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article