Aim: To study the in vivo distribution of N-acetyl-L-glutamic prednisolone (ACEP) and to investigate the renal targeting characteristics of the prodrug.
Methods: The 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.
Results: The concentrations of prednisolone in kidney 15 min after i.v. administration were (86 +/- 8) microgram.g-1 for ACEP group, (57 +/- 4) microgram.g-1 for prednisolone group; 60 min after i.v. administration were (67 +/- 5) microgram.g-1 for ACEP group, (42 +/- 4) microgram.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.
Conclusion: Compared with the parent drug prednisolone, ACEP has kidney-targeting behavior and lower toxicity (n = 5, P < 0.001).