Design, synthesis and preliminary biological evaluations of novel amphiphilic drug carriers

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 14C-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).

Graphical abstractSynthesis and follow-up in mice of a new molecular amphiphilic drug carrier radiolabelled with 14C.Figure optionsDownload full-size imageDownload as PowerPoint slide