Design, synthesis and preliminary biological evaluations of novel amphiphilic drug carriers |
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Authors: | Périno Sandrine Contino-Pépin Christiane Jasseron Sylvain Rapp Maryse Maurizis Jean-Claude Pucci Bernard |
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Institution: | Laboratoire de Chimie Bioorganique et des Systèmes Moléculaires Vectoriels, Faculté des Sciences, 33, rue Louis Pasteur, 84000 Avignon, France. |
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Abstract: | The synthesis of a new fluorocarbon amphiphilic drug carrier is described. A polyfunctional amino acid endowed with a fluorocarbon chain and a sugar moiety providing the amphiphilic character constitutes the central element of this structure. A (14)C-radiolabelled acetyl group was grafted onto the third function and the bioavailability of this molecule was specified in mice after IV administration. This amphiphilic drug carrier exhibits a rapid and homogeneous distribution to the whole tissues and slow elimination half-lives (higher than one day) through a biliary excretion without any toxicity (no measured DL 50 for concentrations up to 500 mg/kg). |
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