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Effect of surface modification on the uptake of polylactic acid nanoparticles loading cyclosporine A by cells in vitro and on the body distribution in vivo

WANG Jie 1, ZHANG Qiang 1, YI Xiang 1, CAO Dong 2, LI Hong Shan 1, WEI Shu Li 1 (1 Department of Pharmaceutics, 2 Department of Pharmacology, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China)  
Objective: To investigate the effect of surface modification on the uptake of cyclosporine A loaded nanoparticles by cells in vitro and on the body distribution in vivo . Methods: The polylactic acid nanoparticles with a mean diameter of 59 nm were prepared with 3H labelled cyclosporine A and then three surfactants: Brij 78, Myrj 53 and Myrj 59 were used to modify the surface of the nanoparticles by physical adsorption. The mouse peritoneal macrophages and 35 mice were used to investigate the uptake of nanoparticles by cells in vitro and body distribution in vivo respectively. Results: In in vitro experiment, a 20 fold increase of cpm value in mouse peritoneal macrophages was observed in cyclosporine A nanoparticles compared with that in the cyclosporine A solution. Surface modification was found to reduce the uptake of nanoparticles. In in vivo body distribution, a noticeable increase of cpm value in reticuloendothelial system (RES) was observed. Conclusion: Surface modification effectively altered the uptake of cyclosporine A loaded polylactic acid nanoparticles by cells in vitro and the body distribution in vivo .
【Fund】: 国家自然科学基金! (39870 897)
【CateGory Index】: R978
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