Table 9. Pharmacokinetic parameters and targeting parameters of GA-S, GA-LP, Gal-GA-LP in plasma and various tissues of mice after i.v. administration (n=5).
Sample | Parameters | Heart | Liver | Spleen | Lung | Kidney | Plasma |
---|---|---|---|---|---|---|---|
GA-S | AUC (μg h L-1) | 3471.481 | 9448.575 | 3217.687 | 4942.941 | 9819.824 | 7373.510 |
Cmax (μg L-1) | 4907.228 | 9485.357 | 6760.000 | 5638.488 | 10764.400 | 5608.573 | |
Te (%) | 9.070 | 24.687 | 8.407 | 12.915 | 25.657 | 19.265 | |
GA-LP | AUC (μg h L-1) | 2654.329 | 20746.629 | 9526.295 | 5918.741 | 5441.211 | 15470.120 |
Cmax (μg L-1) | 5806.441 | 10269.646 | 8819.786 | 9253.503 | 10201.204 | 5403.583 | |
Re | 0.765 | 2.196 | 2.961 | 1.197 | 0.554 | 2.098 | |
Te (%) | 4.442 | 34.718 | 15.942 | 9.905 | 9.106 | 25.888 | |
Ce | 1.183 | 1.083 | 1.305 | 1.641 | 0.948 | 0.963 | |
Gal-GA-LP | AUC (μg h L-1) | 2435.328 | 44901.029 | 6030.967 | 7074.443 | 11202.158 | 21524.930 |
Cmax (μg L-1) | 2479.942 | 26525.004 | 16382.000 | 9888.715 | 14728.002 | 5643.000 | |
Re | 0.702 | 4.752 | 1.874 | 1.431 | 1.141 | 2.919 | |
Te (%) | 2.614 | 48.193 | 6.473 | 7.593 | 12.024 | 23.103 | |
Ce | 0.505 | 2.796 | 2.423 | 1.754 | 1.368 | 1.006 |
Abbreviations: GA-S, glycyrrhetinic acid solvent; GA-LP, glycyrrhetinic acid liposomes; Gal-GA-LP, glycyrrhetinic acid liposomes modified with liver-targeting ligand of galactosylated derivative; AUC, area under concentration-time curve; Re, Relative intake rate; Te, Targeting efficiency; Ce, Peak concentration ratio; i.v., intravascular.