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Abstract
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 99mTc-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.
Acknowledgements
A. Beloqui thanks the University of the Basque Country (UPV/EHU) for her fellowship grant. The authors also thank the Department of Nuclear Medicine at the Hospital Universitario de Canarias (Tenerife, Spain) for their assistance in the biodistribution studies. They also acknowledge the technical support and advice provided by SGIker (UPV/EHU, MICINN, GV/EJ, ESF) on transmission electron microscopy.