[Kidney-targeting characteristics of N-acetyl-L-glutamic prednisolone prodrug].
OBJECTIVE
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.


CONCLUSIONS
Compared with the parent drug prednisolone, ACEP has kidney-targeting behavior and lower toxicity (n = 5, P < 0.001).
Su
Min
M
West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
He
Qin
Q
Zhang
Zhi-rong
ZR
Hu
Bin
B
Liu
Shi-wei
SW
D015502:Absorptiometry, Photon; D000818:Animals; D015519:Bone Density / Q000187:drug effects; D016503:Drug Delivery Systems; D005260:Female; D007668:Kidney / Q000378:metabolism*; D008297:Male; D051379:Mice; D011239:Prednisolone / Q000378:metabolism / Q000493:pharmacokinetics*; D011355:Prodrugs / Q000378:metabolism / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar
D011355:Prodrugs; D011239:Prednisolone