Kidney-targeting characteristics of N-acetyl-L-glutamic prednisolone prodrug

AimTo study the in vivo distribution of N-acetyl-L-glutamic prednisolone (ACEP) and to investigate the renal targeting characteristics of the prodrug. MethodsThe concentrations of prednisolone in organs at predetermined time were assayed by HPLC after intravenous administration of ACEP or prednisolone to Kunming mice. The adverse effects were evaluated by testing the bone mineral densities (BMD) of Wistar rats. ResultsThe concentrations of prednisolone in kidney 15　min after iv administration were (86±8) μg·g^-1 for ACEP group, (57±4) μg·g^-1 for prednisolone group; 60　min after iv administration were (67±5) μg·g^-1 for ACEP group, (42±4) μg·g^-1 for prednisolone group. BMDs were (0.08±0.03) g·cm^-2 and （0.14±0.06） g·cm^-2 for prednisolone and ACEP-treated Wistar rats respectively. ConclusionCompared with the parent drug prednisolone, ACEP has kidney-targeting behavior and lower toxicity (n=5, P<0.001).