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 (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).
Périno
Sandrine
S
Laboratoire de Chimie Bioorganique et des Systèmes Moléculaires Vectoriels, Faculté des Sciences, 33, rue Louis Pasteur, 84000 Avignon, France.
Contino-Pépin
Christiane
C
Jasseron
Sylvain
S
Rapp
Maryse
M
Maurizis
Jean-Claude
JC
Pucci
Bernard
B
D000818:Animals; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics*; D015195:Drug Design; D006207:Half-Life; D008297:Male; D051379:Mice; D015394:Molecular Structure; D049329:Nanostructures; D009368:Neoplasm Transplantation; D013501:Surface-Active Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics
D004337:Drug Carriers; D013501:Surface-Active Agents