title: Formation of bicalutamide nanodispersion for dissolution rate enhancement.
abstract: Bicalutamide was loaded on hydrophilic excipients to form nanodispersions via a combination of anti-solvent precipitation and spray drying method. The particle size, BET surface area, contact angles and dissolution rate of the nanodispersions were analyzed. The results indicated that lactose was a suitable matrix to prevent the bicalutamide particles growth and aggregation. The lactose loaded particles had a mean size of 330 nm within a narrow distribution. X-ray diffraction (XRD), differential scanning calorimetry (DSC) and Fourier transform infrared (FT-IR) characterization indicated the nanodispersion exhibited unchanged crystalline and chemical structure. Dissolution rate of bicalutamide nanodispersion was significantly faster than that of commercial products. It increased to 94% in 10 min while both commercial formulas Casodex and bicalutamide tablets dissolved 60% and 38% respectively at the same period. It was proposed that the enhanced dissolution rate of bicalutamide nanodispersion contribute to high surface area and well-wetted state of drug particles.
authors.affiliation: Key Lab for Nanomaterials, Ministry of Education, Beijing University of Chemical Technology, Beijing 100029, PR China.
authors.forename: Chan
authors.initials: C
authors.lastname: Li
authors.forename: Caixia
authors.initials: C
authors.lastname: Li
authors.forename: Yuan
authors.initials: Y
authors.lastname: Le
authors.forename: Jian-Feng
authors.initials: JF
authors.lastname: Chen
mesh_terms: D000726:Androgen Antagonists / Q000737:chemistry*; D000813:Anilides / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D011232:Chemical Precipitation; D002626:Chemistry, Pharmaceutical; D003460:Crystallization; D018360:Crystallography, X-Ray; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry*; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D007785:Lactose / Q000737:chemistry*; D053758:Nanoparticles; D036103:Nanotechnology; D009570:Nitriles / Q000737:chemistry*; D010316:Particle Size; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods; D013696:Temperature; D014105:Tosyl Compounds / Q000737:chemistry*; D017155:Wettability
chemical_list: D000726:Androgen Antagonists; D000813:Anilides; D005079:Excipients; D009570:Nitriles; D012997:Solvents; D014105:Tosyl Compounds; C053541:bicalutamide; D007785:Lactose