l -Serine–modified polyamidoamine dendrimer as a highly potent renal targeting drug carrier

Significance Delivery of most drug carriers to the kidney is limited because of their uptake by the reticuloendothelial system in the liver and spleen. We have developed l -serine (Ser)–modified polyamidoamine dendrimer (PAMAM) as a potent renal targeting drug carrier for the treatment of kidney diseases. Pharmacokinetic and single-photon emission computed tomography/computed tomography studies indicated that Ser modification results in efficient kidney targeting of PAMAM. Ser-PAMAM accumulated predominantly in proximal tubules, a pattern associated with the pathogenesis of renal cell carcinoma and chronic renal failure. Efficient renal distribution and pharmacologic effect of captopril was observed after i.v. injection of the Ser-PAMAM-captopril conjugate. Thus, our results demonstrate successful kidney targeting of a drug carrier via Ser modification.