Design and synthesis of novel amphiphilic dendritic galactosides for selective targeting of liposomes to the hepatic asialoglycoprotein receptor

…, PJ van Santbrink, MK Bijsterbosch…

Index: Sliedregt, Leo A. J. M.; Rensen, Patrick C. N.; Rump, Erik T.; Van Santbrink, Peter J.; Bijsterbosch, Martin K.; Valentijn, A. Rob P. M.; Van Der Marel, Gijs A.; Van Boom, Jacques H.; Van Berkel, Theo J. C.; Biessen, Erik A. L. Journal of Medicinal Chemistry, 1999 , vol. 42, # 4 p. 609 - 618

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Citation Number: 129

Abstract

A series of glycolipids have been prepared which contain a cluster galactoside moiety with high affinity for the hepatic asialoglycoprotein receptor and a bile acid ester moiety which mediates stable incorporation into liposomes. Loading of liposomes with these glycolipids at a ratio of 5%(w/w) resulted in efficient recognition and uptake of the liposomes by the liver. Preinjection with asialofetuin almost completely inhibited the uptake, establishing that the ...