title: Preparation and characterization of spironolactone-loaded nanocapsules for paediatric use.
abstract: Spironolactone is a steroidal diuretic showing incomplete oral behaviour because of its low solubility and slow dissolution rate. In this study, we applied the nanoprecipitation method to prepare spironolactone-loaded nanocapsules, at laboratory-scale and pilot-scale. The effect of several formulation variables on the spironolactone-loaded nanocapsules properties (average size, drug release rate and drug entrapment) was investigated. The optimized formulations at laboratory-scale and pilot-scale lead to the preparation of spironolactone-loaded nanocapsules with a mean size of 320 and 400 nm, respectively, a high encapsulation efficiency (96.21% and 90.56% respectively), both stable for 6 months. The release of spironolactone from nanocapsules was rapid and complete in a simulated gastric fluid, therefore recourse to spironolactone nanoencapsulation should enhance its oral bioavailability and probably its efficiency. The optimized formulations lead to a high drug-concentration in the liquid preparation (1.5 mg/ml) allowing minimizing the preparation volume administered for children medication.
authors.affiliation: Laboratoire d'Automatique et de Génie des Procédés (LAGEP), UMR-CNRS 5007, CPE Lyon, Université Claude Bernard Lyon 1, Bât 308 G, 43 Boulevard du 11 Novembre 1918, F-69622 Villeurbanne Cedex, France. limayem@lagep.univ-lyon.fr
authors.forename: I
authors.initials: I
authors.lastname: Limayem Blouza
authors.forename: C
authors.initials: C
authors.lastname: Charcosset
authors.forename: S
authors.initials: S
authors.lastname: Sfar
authors.forename: H
authors.initials: H
authors.lastname: Fessi
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004339:Drug Compounding / Q000295:instrumentation / Q000379:methods*; D004355:Drug Stability; D004356:Drug Storage; D046529:Microscopy, Electron, Transmission / Q000379:methods; D008970:Molecular Weight; D053769:Nanocapsules / Q000737:chemistry* / Q000648:ultrastructure; D036103:Nanotechnology / Q000295:instrumentation / Q000379:methods; D009821:Oils / Q000737:chemistry / Q000145:classification; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry; D011091:Polyesters / Q000737:chemistry; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D013148:Spironolactone / Q000737:chemistry / Q000493:pharmacokinetics*; D013997:Time Factors
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D053769:Nanocapsules; D009821:Oils; D011091:Polyesters; D012997:Solvents; D020442:Poloxamer; C016240:polycaprolactone; D013148:Spironolactone