title: Enhanced bioavailability of raloxifene hydrochloride via dry suspensions prepared from drug/HP-β-cyclodextrin inclusion complexes.
abstract: This study aimed to develop a dry suspension formulation of raloxifene (RLX) using its HP-β-cyclodextrin inclusion complexes to enhance the oral bioavailability. Dry suspensions loading RLX/HP-β-cyclodextrin inclusion complexes (RLX-HICs) were prepared by solvent evaporation followed by a standard wet granulation process. The inclusion complexes were characterized by scanning electron microscopy, differential scanning calorimetry, and Fourier transform infrared spectroscopy. The features of dry suspensions such as dispersibility, flowability and dissolution were compared with conventional suspensions. Dry suspensions containing RLX-HICs dramatically increased the dissolution of RLX. Pharmacokinetic studies in rats showed that dry suspensions with RLX-HICs significantly enhanced the oral bioavailabilities of RLX. The absolute and relative bioavailabilities were up to 13.04% and 413.97% compared with the solution formulation (i.v.) and conventional suspensions (i.g.), respectively. The bioavailability improvement for dry suspensions with RLX-HICs can be attributed to improved dissolution and physiochemical properties of RLX, by which the overall absorption was enhanced. Dry suspensions prepared from RLX-HICs may be an attractive formulation for the oral delivery of RLX.
authors.forename: Rong
authors.initials: R
authors.lastname: Lu
authors.forename: Shan
authors.initials: S
authors.lastname: Liu
authors.forename: Qilin
authors.initials: Q
authors.lastname: Wang
authors.forename: Xia
authors.initials: X
authors.lastname: Li
mesh_terms: D000818:Animals; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D004339:Drug Compounding; D016503:Drug Delivery Systems; D008855:Microscopy, Electron, Scanning; D008958:Models, Molecular; D020849:Raloxifene Hydrochloride / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D020845:Selective Estrogen Receptor Modulators / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013535:Suspensions; D047392:beta-Cyclodextrins / Q000737:chemistry
chemical_list: D020845:Selective Estrogen Receptor Modulators; D013535:Suspensions; D047392:beta-Cyclodextrins; D020849:Raloxifene Hydrochloride