title: Loteprednol Etabonate Nanoparticles: Optimization via Box-Behnken Design Response Surface Methodology and Physicochemical Characterization.
abstract: BACKGROUND
  Abstract: The objective of the present work was to prepare and optimize the loteprednoletabonate (LE) loaded poly (D,L-lactide co-glycolide) (PLGA) polymer based nanoparticle carrier. The review on recent patents (US9006241, US20130224302A1, US2012/0028947A1) assisted in the selection of drug and polymer for designing nanoparticles for ocular delivery applications.
  
  
  METHODS
  The nanoparticles were prepared by solvent evaporation followed by high speed homogenization. Biodegradable polymer PLGA (50:50) grade was utilized to develop various formulations with different drug:polymer ratio. A Box-Behnken design with 33 factorial design was selected for the present study and 17 runs were carried out in totality. The influence of various process variables (viz., polymer concentration, homogenization speed and sonication time) on the characteristics of nanoparticles including the in vitro drug release profile were studied.
  
  
  RESULTS
  The nanoparticulate formulations were evaluated for mean spherical diameter, polydispersity index (PDI), zeta potential, surface morphology, drug entrapment and in-vitro drug release profile. The entrapment efficiency, drug loading and mean particle size were found to be 96.31±1.68 %, 35.46±0.35 % and 167.6±2.1 nm respectively.
  
  
  CONCLUSIONS
  The investigated process and formulation variables were found to have significant effect on the particle size, drug loading (DL), entrapment efficiency (EE), and in vitro drug release profile. A biphasic in vitro drug release profile was apparent from the optimized nanoparticles (NPs) for 24 hours.
authors.affiliation: University Institute of Pharmacy, Faculty of Technology, Pt. Ravishankar Shukla University, Raipur-492010, Chhattisgarh, India.
authors.forename: Abhishek K
authors.initials: AK
authors.lastname: Sah
authors.affiliation: University Institute of Pharmacy, Faculty of Technology, Pt. Ravishankar Shukla University, Raipur-492010, Chhattisgarh, India.
authors.forename: Preeti K
authors.initials: PK
authors.lastname: Suresh
mesh_terms: D060433:Administration, Ophthalmic; D004337:Drug Carriers; D065546:Drug Liberation; D019344:Lactic Acid; D000069559:Loteprednol Etabonate / Q000737:chemistry*; D053758:Nanoparticles; D010316:Particle Size; D011100:Polyglycolic Acid; D011108:Polymers
chemical_list: D004337:Drug Carriers; D011108:Polymers; D011100:Polyglycolic Acid; D019344:Lactic Acid; D000069559:Loteprednol Etabonate
keywords: Box-behnken design; PLGA; corticosteroid; loteprednol etabonate; nanoparticle; ocular delivery; optimization; surface
  response methodology