title: [Relative bioavailability of cyclosporine A-loaded hydroxypropyl methylcellulose phthalate nanoparticles for oral administration in rats].
abstract: OBJECTIVE
  To study the preparation of hydroxypropyl methylcellulose phthalate (HPMCP) nanoparticles and compare its pharmacokinetic characteristics with Neoral.
  
  
  METHODS
  HPMCP nanoparticles loaded cyclosporine A were prepared by solvent-nonsolvent method. CyA-HP50 nanoparticles, CyA-HP55 nanoparticles and Neoral were orally administered at the dosage of 15 mg x kg(-1) to rats. The CyA concentration in blood were determined by HPLC. Pharmacokinetic parameters were calculated by 3P97 program.
  
  
  RESULTS
  The concentration-time data of the three preparations were best fit by two compartment model. The relative bioavailability of CyA-HP50 and CyA-HP55 nanoparticles calculated by the AUC0-72 were 82.3% and 119.6%, bioequivalent to the reference of Neoral. The relative bioavailability of CyA-HP55 nanoparticles was 145.3% of CyA-HP50 nanoparticles.
  
  
  CONCLUSIONS
  CyA HPMCP nanoparticles could be prepared easily and reproducibly. It was found that the oral absorption of CyA can be increased by using the HPMCP nanoparticles.
authors.affiliation: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China.
authors.forename: Xue-qing
authors.initials: XQ
authors.lastname: Wang
authors.forename: Jun-dong
authors.initials: JD
authors.lastname: Dai
authors.forename: Qiang
authors.initials: Q
authors.lastname: Zhang
authors.forename: Tao
authors.initials: T
authors.lastname: Zhang
authors.forename: Gui-min
authors.initials: GM
authors.lastname: Xia
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D016572:Cyclosporine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D007166:Immunosuppressive Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008297:Male; D008747:Methylcellulose / Q000008:administration & dosage* / Q000031:analogs & derivatives*; D049329:Nanostructures; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D007166:Immunosuppressive Agents; D016572:Cyclosporine; D008747:Methylcellulose; C053309:hydroxypropyl methylcellulose phthalate