Preparation and characterization of spironolactone-loaded nanocapsules for paediatric use

Int J Pharm. 2006 Nov 15;325(1-2):124-31. doi: 10.1016/j.ijpharm.2006.06.022. Epub 2006 Jun 23.

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.

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
  • Chemistry, Pharmaceutical / methods
  • Drug Compounding / instrumentation
  • Drug Compounding / methods*
  • Drug Stability
  • Drug Storage
  • Microscopy, Electron, Transmission / methods
  • Molecular Weight
  • Nanocapsules / chemistry*
  • Nanocapsules / ultrastructure
  • Nanotechnology / instrumentation
  • Nanotechnology / methods
  • Oils / chemistry
  • Oils / classification
  • Particle Size
  • Poloxamer / chemistry
  • Polyesters / chemistry
  • Solubility
  • Solvents / chemistry
  • Spironolactone / chemistry
  • Spironolactone / pharmacokinetics*
  • Time Factors

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Nanocapsules
  • Oils
  • Polyesters
  • Solvents
  • Poloxamer
  • polycaprolactone
  • Spironolactone