Organ distribution of 5-fluorouracil loaded gelatine microspheres in mice
Hao, X.; Cheng, G.; Zou, M.; Sun, J.; Cui, F.
Die Pharmazie 59(9): 709-712
2004
ISSN/ISBN: 0031-7144 PMID: 15497754 Document Number: 584207
The aim of this study was to investigate the organ distribution characteristics of 5-fluorouracil (5-Fu) loaded crosslinked gelatine microspheres (5-Fu-MS) after intravenous (i.v.) injection compared to 5-Fu solution in mice, and to evaluate the targetability of 5-Fu-MS. The concentrations of 5-Fu in mice plasma, heart, liver, lung, kidney, spleen and brain were determined by HPLC. The parameters drug targeting index Ce, time-averaged relative drug exposure values re, drug targeting efficiency te, and drug distributed to target-tissue (%) were used to evaluate the targetability of the 5-Fu-MS delivery system. The results showed that the concentration of 5-Fu in the lung was significantly higher than after application of 5-Fu solution, and that the maximum concentration of 5-Fu, 72.8 mug. g organ-1, was reached in the lung at 15 min after i.v. administration. As for 5-Fu-MS, re was calculated to be 2.2, and te was considerably higher than after application of 5-Fu in solution. Furthermore, the percentage of drug distributed to the lung was 2 times as high as after application in solution. Accordingly, 5-Fu-MS were capable of effectively delivering 5-Fu to the lung and possessed specific targetability towards the lung compared to 5-Fu solution.