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7417908 
Journal Article 
Targeted drug delivery to renal proximal tubule epithelial cells mediated by 2-glucosamine 
Lin, Y; Li, Y; Wang, X; Gong, T; Zhang, L; Sun, X; , 
2013 
Yes 
Journal of Controlled Release
ISSN: 0168-3659
EISSN: 1873-4995 
ELSEVIER SCIENCE BV 
AMSTERDAM 
167 
2 
148-156 
English 
23415893 
WOS:000316678400005 
In order to develop a novel kidney-targeted drug delivery system, we synthesized prednisolone carbamate-glucosamine conjugate (PCG) using 2-glucosamine as a ligand, and investigated its potential targeting efficacy. In vitro studies demonstrated that PCG could remarkably improve the uptake of drug by kidney cells. And the specific uptake of PCG could be largely reduced by the inhibitors of megalin receptor. More importantly, PCG showed an excellent kidney targeting property in vivo, and the concentration of the conjugate in the kidney was 8.1-fold higher than that of prednisolone group at 60 min after intravenous injection. Besides, PCG could significantly reverse the disease progression in renal ischemia-reperfusion (I/R) injury animal models. Furthermore, PCG presented no adverse effect on bone density while prednisolone resulted in severe osteoporosis. Thus, it indicated that 2-glucosamine could be a potential ligand for kidney-targeted delivery of prednisolone. 
Glucosamine; Kidney-targeting; Megalin; Prednisolone; Uptake; Intravenous injections; Ischemia reperfusion; Kidney-targeting; Megalin; Prednisolone; Targeted drug delivery; Targeting efficacies; Uptake; Drug delivery; Ligands; Glucosamine; 2 glucosamine; carbamic acid; glucosamine derivative; megalin; prednisolone; prednisolone carbamate glucosamine conjugate; prednisolone derivative; unclassified drug; animal cell; animal experiment; animal model; animal tissue; article; bone density; conjugate; controlled study; disease course; disease model; drug delivery system; drug uptake; epithelium cell; human; human cell; in vitro study; in vivo study; kidney proximal tubule; male; mouse; nonhuman; osteoporosis; priority journal; rat; reperfusion injury; single drug dose; Acute Kidney Injury; Animals; Anti-Inflammatory Agents; Bone Density; Carbamates; Cell Line; Epithelial Cells; Glucosamine; Humans; Kidney Tubules, Proximal; Male; Prednisolone; Rats; Rats, Sprague-Dawley; Reperfusion Injury; Tissue Distribution 
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