Enhanced drug loading in polymerized micellar cargo.
A new drug carrier system based on self-assembly and polymerization of polydiacetylenic amphiphiles is described. Although classical amphiphiles can help in solubilizing hydrophobic molecules upon self-arrangement into a variety of nanometric structures, a greater effect on drug loading was observed for our polymerized micelles as compared to the non-polymerized analogues. This permitted higher aqueous solubilization of lipophilic drugs with low micelle concentration. (14)C labeling of a model drug on one side and of the amphiphile on the other side permitted assessment, after intravenous injection, of biodistribution and excretion profiles of the drug cargo.
Ogier
Julien
J
CEA, iBiTecS, Service de Chimie Bioorganique et de Marquage, 91191 Gif-sur-Yvette, France.
Arnauld
Thomas
T
Carrot
Géraldine
G
Lhumeau
Antoine
A
Delbos
Jean-Marie
JM
Boursier
Claire
C
Loreau
Olivier
O
Lefoulon
Francois
F
Doris
Eric
E
D000818:Animals; D057927:Hydrophobic and Hydrophilic Interactions; D008297:Male; D051379:Mice; D008823:Micelles; D046529:Microscopy, Electron, Transmission; D015394:Molecular Structure; D000078789:Polyacetylene Polymer; D011108:Polymers / Q000737:chemistry* / Q000378:metabolism; D053279:Polyynes / Q000737:chemistry* / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility
D008823:Micelles; D000078789:Polyacetylene Polymer; D011108:Polymers; D053279:Polyynes; C082361:polydiacetylene