Relative bioavailability of cyclosporine A-loaded hydroxypropyl methylcellulose phthalate nanoparticles for oral administration in rats.
- Author:
Xue-qing WANG
1
;
Jun-dong DAI
;
Qiang ZHANG
;
Tao ZHANG
;
Gui-min XIA
Author Information
- Publication Type:Journal Article
- MeSH: Administration, Oral; Animals; Area Under Curve; Biological Availability; Cyclosporine; administration & dosage; pharmacokinetics; Immunosuppressive Agents; administration & dosage; pharmacokinetics; Male; Methylcellulose; administration & dosage; analogs & derivatives; Nanostructures; Particle Size; Rats; Rats, Sprague-Dawley
- From: Acta Pharmaceutica Sinica 2004;39(6):463-466
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo study the preparation of hydroxypropyl methylcellulose phthalate (HPMCP) nanoparticles and compare its pharmacokinetic characteristics with Neoral.
METHODSHPMCP 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.
RESULTSThe 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.
CONCLUSIONCyA 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.
