Lipids-based nanostructured lipid carriers (NLCs) for improved oral bioavailability of sirolimus.
Drug Deliv
; 23(4): 1469-75, 2016 May.
Article
en En
| MEDLINE
| ID: mdl-27187522
ABSTRACT
The main purpose of this study was to improve the oral bioavailability of sirolimus (SRL), a poorly water-soluble immunosuppressant, by encapsulating into lipids-based nanostructured lipid carriers (NLCs). SRL-loaded NLCs (SRL-NLCs) were prepared by a high-pressure homogenization method with glycerol distearates (PRECIROL ATO-5) as the solid lipid, oleic acid as the liquid lipids, and Tween 80 as the emulsifier. The SRL-NLCs prepared under optimum conditions was spherical in shape with a mean particle size of about 108.3 nm and an entrapment efficiency of 99.81%. In vitro release of SRL-NLCs was very slow, about 2.15% at 12 h, while in vitro lipolysis test showed fast digestion of the NLCs within 1 h. Relative oral bioavailability of SRL-NLCs in Beagle dogs was 1.81-folds that of the commercial nanocrystalline sirolimus tablets Rapamune®. In conclusion, the NLCs show potential to improve the oral bioavailability of SRL.
Palabras clave
Texto completo:
1
Base de datos:
MEDLINE
Asunto principal:
Portadores de Fármacos
/
Sirolimus
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Nanopartículas
/
Lípidos
Idioma:
En
Revista:
Drug Deliv
Asunto de la revista:
FARMACOLOGIA
/
TERAPIA POR MEDICAMENTOS
Año:
2016
Tipo del documento:
Article