title: Bicalutamide nanocrystals with improved oral bioavailability: in vitro and in vivo evaluation.
abstract: BACKGROUND
  Bicalutamide (BCT) is an antiandrogenic compound belonging to Biopharmaceutics Classification System (BCS) class II drug. Thus it has limited aqueous solubility and hence limited oral bioavailability.
  
  
  OBJECTIVE
  The purpose of the present investigation was to obtain stable nanocrystals of BCT with improved kinetic solubility, dissolution and pharmacokinetic profiling.
  
  
  METHODS
  BCT nanocrystals were prepared by antisolvent precipitation method using Soluplus, a novel amphiphilic polymer. Nanocrystals were characterized for particle size, powder X-ray diffraction analysis (PXRD), in vitro dissolution, in vivo pharmacokinetic profile and stability.
  
  
  CONCLUSIONS
  The obtained nanocrystals had particle size of 168 nm and were spherical in shape. The nanocrystals exhibited fivefold increase in kinetic solubility as compared to pure drug and 85% dissolution in 60 min. PXRD studies established the retention of crystalline polymorphic form II. The in vivo pharmacokinetic study demonstrated that the Cmax and AUC of nanosized BCT were about 3.5 times higher as compared to pure drug.
  
  
  CONCLUSIONS
  Nanosizing of BCT significantly improved the pharmacokinetic profile of the drug administered to rats. Prepared nanocrystals were found to be stable over the entire stability period. Thus the use of amphiphilic polymer like Soluplus singularly helped in efficient size reduction and stabilization of the drug.
authors.affiliation: Department of Pharmaceutics, Bharati Vidyapeeth University, Poona College of Pharmacy, Erandwane, Pune, Maharashtra, India. vbpokharkar@yahoo.co.in
authors.forename: Varsha B
authors.initials: VB
authors.lastname: Pokharkar
authors.forename: Tripti
authors.initials: T
authors.lastname: Malhi
authors.forename: Leenata
authors.initials: L
authors.lastname: Mandpe
mesh_terms: D000284:Administration, Oral; D000813:Anilides / Q000008:administration & dosage* / Q000097:blood* / Q000493:pharmacokinetics; D000818:Animals; D001682:Biological Availability; D011232:Chemical Precipitation; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage*; D009570:Nitriles / Q000008:administration & dosage* / Q000097:blood* / Q000493:pharmacokinetics; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D014105:Tosyl Compounds / Q000008:administration & dosage* / Q000097:blood* / Q000493:pharmacokinetics; D014961:X-Ray Diffraction
chemical_list: D000813:Anilides; D009570:Nitriles; D014105:Tosyl Compounds; C053541:bicalutamide