Prodrug approaches for enhancing the bioavailability of drugs with low solubility.
Low water solubility and low bioavailability are frequent problems in drug development, particularly in the area of central nervous system (CNS) drugs. This short review describes selected prodrug approaches which have been developed to enhance the bioavailability of drugs, especially that of poorly soluble drugs. Some of the most successful drugs on the market are prodrugs. With a better understanding of active-transport processes at cell membranes in the gut as well as at the blood-brain barrier, the importance of prodrug approaches will further increase in the future. Prodrug approaches will already be considered in the early phase of drug discovery.
Müller
Christa E
CE
PharmaCenter Bonn, University of Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, An der Immenburg 4, D-53121 Bonn. christa.mueller@uni-bonn.de
D000818:Animals; D001682:Biological Availability; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D006801:Humans; D008055:Lipids / Q000737:chemistry; D004364:Pharmaceutical Preparations / Q000737:chemistry* / Q000378:metabolism*; D011355:Prodrugs / Q000493:pharmacokinetics*; D012995:Solubility; D014867:Water
D008055:Lipids; D004364:Pharmaceutical Preparations; D011355:Prodrugs; D014867:Water