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Fate of nanostructured lipid carriers (NLCs) following the oral route: design, pharmacokinetics and biodistribution

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Beloqui Garcia, Ana [UCL] Solinís, María Ángeles Delgado, Araceli Evora, Carmen Isla, Arantxazu Rodríguez-Gascón, Alicia

The aim of this study was to develop a nanostructured lipid carriers (NLC) formulation containing spironolactone (SPN-NLCs), and to investigate its potential for the oral delivery of poorly water-soluble compounds. SPN-NLCs were orally administered to rabbits and the pharmacokinetics of spironolactone and its metabolites was evaluated. As reference formulation, we administered syrup. Spironolactone was only detected in a few plasma samples; hence, metabolite levels were employed for the pharmacokinetic analysis. The absolute bioavailability of 7α-TMS was significantly higher with the syrup than those obtained with the SPN-NLCs (0.7 versus 0.4, p < 0.05). However, no significant differences were observed in the bioavailability of canrenone, revealing a different canrenone/7α-TMS ratio depending on the administered formulation. Orally administered (99m)Tc-radiolabeled SPN-NLCs were mainly detected in the small intestine. These results suggest the retention of the nanocarriers in the underlying epithelium and further uptake by the epithelial cells.

Document type Article de périodique (Journal article) – Article de recherche
Access type Accès restreint
Publication date 2014
Language Anglais
Journal information "Journal of Microencapsulation" - Vol. 31, no. 1, p. 1-8 (2014)
Peer reviewed yes
Publisher Informa Healthcare ((United Kingdom) London)
issn 0265-2048
e-issn 1464-5246
Publication status Publié
Affiliation UCL - SSS/LDRI - Louvain Drug Research Institute
MESH Subject Administration, Oral ; Animals ; Diuretics ; Drug Carriers ; Lipids ; Male ; Nanostructures ; Rabbits ; Spironolactone
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Bibliographic reference Beloqui Garcia, Ana ; Solinís, María Ángeles ; Delgado, Araceli ; Evora, Carmen ; Isla, Arantxazu ; et. al. Fate of nanostructured lipid carriers (NLCs) following the oral route: design, pharmacokinetics and biodistribution. In: Journal of Microencapsulation, Vol. 31, no. 1, p. 1-8 (2014)
Permanent URL http://hdl.handle.net/2078.1/154637