[Study on preparation conditions for polylactide nanoparticles loaded cyclosporine A and its oral bioavailability in rats].
OBJECTIVE
To develop a less toxic alternative for sandimmun neoral (Neoral). To study the preparation conditions and to compare its pharmacokinetic characteristics with Neoral.


METHODS
Polylactide nanoparticles loaded cyclosporine A was prepared by solvent-nonsolvent method. Polylactide nanoparticles were administered by oral in a dosage of 15 mg.kg-1. The CyA concentration in whole blood sample was determined by HPLC.


RESULTS
The quantities of CyA, PLA and volume of acetone added had significant influence on the NP diameters. Under proper condition, the nanoparticles with diameters of 57.5 nm were obtained. The relative bioavailability in rats was 101.6%, with a smaller absorption rate (P < 0.05) and a smaller elimination rate (P < 0.1).


CONCLUSIONS
The nanoparticles (diamater < 100 nm) with relative high bioavailability were prepared using solvent-nonsolvent method. It is suitable for further study.
Wang
Xue-qing
XQ
Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China.
Zhang
Tao
T
He
Ying
Y
Zhang
Liang
L
Zhang
Qiang
Q
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D016572:Cyclosporine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D003692:Delayed-Action Preparations; D007166:Immunosuppressive Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008297:Male; D036103:Nanotechnology; D011091:Polyesters; D011897:Random Allocation; D051381:Rats; D017208:Rats, Wistar
D003692:Delayed-Action Preparations; D007166:Immunosuppressive Agents; D011091:Polyesters; C033616:poly(lactide); D016572:Cyclosporine