title: Fate of nanostructured lipid carriers (NLCs) following the oral route: design, pharmacokinetics and biodistribution.
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 (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.
authors: Pharmacokinetics, Nanotechnology and Gene Therapy Group, Laboratory of Pharmacy and Pharmaceutical Technology, School of Pharmacy, University of the Basque Country (UPV/EHU) , Vitoria-Gasteiz , Spain and.
authors: Ana
authors: A
authors: Beloqui
authors: María Ángeles
authors: MÁ
authors: Solinís
authors: Araceli
authors: A
authors: Delgado
authors: Carmen
authors: C
authors: Evora
authors: Arantxazu
authors: A
authors: Isla
authors: Alicia
authors: A
authors: Rodríguez-Gascón
mesh_terms: D000284:Administration, Oral; D000818:Animals; D004232:Diuretics / Q000493:pharmacokinetics / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D008055:Lipids / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D008297:Male; D049329:Nanostructures / Q000737:chemistry*; D011817:Rabbits; D013148:Spironolactone / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D004232:Diuretics; D004337:Drug Carriers; D008055:Lipids; D013148:Spironolactone