Preparation of cyclosporine A pH sensitive nanoparticles and oral pharmacokinetics in rats

To study the preparation conditions and its oral pharmacokinetic characteristics of cyclosporine A (CyA) pH sensitive nanoparticles. The CyA pH sensitive nanoparticles were prepared by the quasi-emulsion solvent diffusion technique (QESD). Male Sprague-Dawley (SD) rats weighing (250 +/- 20) g were s...

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Bibliographic Details
Published inYao hsüeh hsüeh pao Vol. 39; no. 12; p. 1023
Main Authors Dai, Jun-dong, Wang, Xue-qing, Zhang, Tao, Meng, Meng, Zhang, Xuan, Lü, Wan-liang, Zhang, Qiang
Format Journal Article
LanguageChinese
Published China 01.12.2004
Subjects
Administration, Oral
Animals
Area Under Curve
Biological Availability
Cyclosporine - administration & dosage
Cyclosporine - pharmacokinetics
Hydrogen-Ion Concentration
Male
Nanostructures
Random Allocation
Rats
Rats, Sprague-Dawley
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Summary:To study the preparation conditions and its oral pharmacokinetic characteristics of cyclosporine A (CyA) pH sensitive nanoparticles. The CyA pH sensitive nanoparticles were prepared by the quasi-emulsion solvent diffusion technique (QESD). Male Sprague-Dawley (SD) rats weighing (250 +/- 20) g were selected and randomly divided into five groups. The bioavailability of CyA from nanoparticles and Neoral microemulsion were assessed at a dose of 15 mg x kg(-1) by gavage. The concentration of CyA in whole blood samples was detected by HPLC to evaluate the relative bioavailability of CyA pH sensitive nanoparticles. The blood concentration profiles of CyA pH sensitive nanoparticles in rats fitted to two compartment models using 3P87 pharmacokinetic calculation program. Compared with the Neoral microemulsion, the relative bioavailability of CyA was 94.8%, 115.2%, 113.6% and 132.5% for CyA-E100, CyA-L100, CyA-L100-55 and CyA-S100 nanoparticles respectively. CyA-S100 nanoparticles was shown to significantly improve the
ISSN:0513-4870