Submitted on April 13, 2005
Revised on August 25, 2005
Accepted on August 27, 2005
Synthesis of phospholipid conjugated bile salts and the suitability of bile salt coated liposomes for interaction with cultured hepatocytes
Gerhard Putz, Wolfgang Schmider, Roland Nitschke, Gerhard Kurz, and Hubert E. Blum
Clinical Chemistry, Universitaetsklinikum Freiburg, Freiburg 79106
Corresponding Author: puetz{at}medizin.ukl.uni-freiburg.de
This paper investigates the possibility of targeting liposomes to hepatocytes via bile salts. The bile salt lithocholyltaurine was covalently linked to a phospholipid and bile salt bearing liposomes (BSL) were prepared. Binding of BSL to rat hepatocytes in primary culture was measured by confocal laser scanning microscopy and H3-labelled liposomes. Interaction of BSL with hepatocyte specific transport systems for cholyltaurine was shown by inhibition of cholyltaurine uptake. The influence of cholyltaurine on the binding of BSL showed a complex character probably due to regulatory processes. The conformation of the 3-position of the bile salt, linking the bile salt and the phospholipid, has a major influence on the interaction between BSL and hepatocytes. In general, bile salts may be suitable ligands for the targeting of liposomes to hepatocytes.
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