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In order to develop a novel kidney-targeted drug delivery system, a small molecular carrier (2-deoxy-2-aminodiglucose) was synthesized, and then the 2-deoxy-2-aminodiglucose–prednisolone conjugate (DPC) was synthesized to verify the kidney targeting capability of the carrier. Both 2-deoxy-2-aminodiglucose and DPC were confirmed by NMR and MS spectrum. The tissue distribution studies showed that DPC presented an excellent kidney targeting property in vivo, compared with prednisolone group, 4.9-fold of drug concentration in kidney was observed in the DPC group. Thus, it indicated that 2-deoxy-2-aminodiglucose could be a potential carrier for kidney-targeted drug delivery.

Prednisolone succinate–glucosamine (PSG) conjugate, a prodrug for prednisolone, was synthesized and confirmed by NMR and MS spectrum. The stabilities of the prodrug in PBS (pH 2.50, 5.00, 7.20, and 7.89) were studied. Cytotoxicity and uptake assay of the prodrug were perfomed on HK-2 and MDCK cell lines. The results showed that compared with prednisolone, the PSG not only did not increase the cytotoxicity but also improved the uptake to 2.2 times of prednisolone by the cells. Thus, it indicated that glucosamine might be a potential carrier for kidney-targeting delivery of prednisolone.