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Relative bioavailability of cyclosporine A-loaded hydroxypropyl methylcellulose phthalate nanoparticles for oral administration in rats

Wang, X-qing.; Dai, J-dong.; Zhang, Q.; Zhang, T.; Xia, G-min.

Yao Xue Xue Bao 39(6): 463-466

2004

ISSN/ISBN: 0513-4870
PMID: 15491107
Document Number: 575875
Aim 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 . 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. Conclusion 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.

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