Lipophilic Derivatization of the Antiviral Drug 9-(2-Phosphonylmethoxyethyl)adenine and Its Incorporation into a Lactosylated Lipid Carrier to Improve Its Liver Uptake

Remco L.A. de Vrueh Division of Biopharmaceutics, Leiden/Amsterdam Center for Drug Research, Leiden University, P.O.Box 9503, 2300, RA, Leiden, The Netherlands

Erik T. Rump Division of Biopharmaceutics, Leiden/Amsterdam Center for Drug Research, Leiden University, P.O.Box 9503, 2300, RA, Leiden, The Netherlands

Erik A.L. Biessen Division of Biopharmaceutics, Leiden/Amsterdam Center for Drug Research, Leiden University, P.O.Box 9503, 2300, RA, Leiden, The Netherlands

Jan Balzarini Laboratory of Virology and Experimental Chemotherapy, Rega-Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroederstraat 10, B-3000, Leuven, Belgium

Theo J.C. van Berkel Division of Biopharmaceutics, Leiden/Amsterdam Center for Drug Research, Leiden University, P.O.Box 9503, 2300, RA, Leiden, The Netherlands

Martin K. Bijsterbosch Division of Biopharmaceutics, Leiden/Amsterdam Center for Drug Research, Leiden University, P.O.Box 9503, 2300, RA, Leiden, The Netherlands

Abstract

Lipophilic derivatization of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) with lithocholic acid-3-oleate and its subsequent incorporation into a lactosylated lipid carrier was found to substantially increase uptake of the drug by the liver. Competition experiments with asialofetuin point to a major role of the parenchymal liver cell, the main site of hepatitis B virus infection.

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Lipophilic Derivatization of the Antiviral Drug 9-(2-Phosphonylmethoxyethyl)adenine and Its Incorporation into a Lactosylated Lipid Carrier to Improve Its Liver Uptake

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Lipophilic Derivatization of the Antiviral Drug 9-(2-Phosphonylmethoxyethyl)adenine and Its Incorporation into a Lactosylated Lipid Carrier to Improve Its Liver Uptake

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