Strategies to increase the oral bioavailability of nucleoside analogs.
Nucleoside analogs are first line chemotherapy in various severe diseases: AIDS (acquired immunodeficiency disease syndrome), cytomegalovirus infections, cancer etc. However, most of these compounds suffer from poor bioavailability via oral route. In order to get around this drawback, researchers have imagined many strategies including drug metabolism inhibitors, bio adhesive nanoparticles, amino ester prodrugs, as well as enhancing absorption by increasing drug lipophilicity. This paper illustrated these approaches by developing their application to some nucleoside analogs. Moreover, some of these strategies were very successful and some resulting compounds are now approved by FDA (Food and Drug Administration).
Univ Paris-Sud, UMR 8612, IFR 141, F-92296 Châtenay-Malabry, CNRS, UMR 8612, IFR 141, F-92296 Châtenay-Malabry, France.
Muriel
M
Lalanne
Karine
K
Andrieux
Patrick
P
Couvreur
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D016503:Drug Delivery Systems / Q000379:methods*; D004791:Enzyme Inhibitors / Q000008:administration & dosage* / Q000378:metabolism; D006801:Humans; D008055:Lipids / Q000737:chemistry; D026901:Membrane Transport Proteins / Q000378:metabolism; D053758:Nanoparticles / Q000737:chemistry; D009705:Nucleosides / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics*
D004791:Enzyme Inhibitors; D008055:Lipids; D026901:Membrane Transport Proteins; D009705:Nucleosides; C043912:peptide permease