title: Quality by design approach to understand the process of optimization of iloperidone nanostructured lipid carriers for oral bioavailability enhancement.
abstract: BACKGROUND
  The current work was carried out by exploring the principles of quality by design approach to develop an optimized nanostructured lipid carrier (NLC) formulation of poorly water soluble active iloperidone (ILO) through systematic statistical study. The potential of NLC for improving the oral bioavailability of ILO was also evaluated.
  
  
  OBJECTIVE
  To understand the effect of formulation variables (critical parameters) on the performance characteristics (critical quality attributes) of NLC.
  
  
  METHODS
  A 3-factor, 3-level Box-Behnken factorial design was explored to predict the responses such as particle size (Y1) and % entrapment efficiency (EE) (Y2) when concentration of lipid (X1), concentration of drug (X2) and concentration of surfactant (X3) were selected as independent variables.
  
  
  CONCLUSIONS
  Particle size analysis revealed that all the batches were within the nanometer range. The % EE was found to be between 63% and 96%. In-vitro release study demonstrated sustained release profile of ILO NLC. The pharmacokinetic study in Wistar rats over the period of 24 h demonstrated 8.30-fold increase in oral bioavailability of ILO NLC as compared with ILO pure drug suspension.
  
  
  CONCLUSIONS
  The NLC formulation remarkably improved the oral bioavailability of ILO and demonstrated a promising perspective for oral delivery of poorly water-soluble drugs.
authors: Department of Pharmaceutics, Poona College of Pharmacy, Bharati Vidyapeeth University , Pune, Maharashtra , India.
authors: Leenata
authors: L
authors: Mandpe
authors: Varsha
authors: V
authors: Pokharkar
mesh_terms: D000284:Administration, Oral; D000818:Animals; D014150:Antipsychotic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D007555:Isoxazoles / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D008055:Lipids / Q000737:chemistry*; D008297:Male; D053758:Nanoparticles; D010316:Particle Size; D010880:Piperidines / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry
chemical_list: D014150:Antipsychotic Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D007555:Isoxazoles; D008055:Lipids; D010880:Piperidines; D013501:Surface-Active Agents; C081732:iloperidone
keywords: Box–Behnken design; factorial design; relative bioavailability