Delivery aspects of small peptides and substrates for peptide transporters.
The present summary highlight chemical strategies applied to improve plasma half-lives and oral bioavailability of peptidic drugs as well as view on intestinal and pancreatic peptidase mediated degradation of peptidic drugs. In general chemical strategies used to increase the oral bioavailability of peptidic drugs consisting of more than three amino acids is disappointing. On the other hand chemical approaches to stabilize peptidic drugs against metabolism seem promising for increasing plasma half-lives of parental peptidic drugs as well as for increasing oral bioavailability of di/tripeptidomimetics and dipeptidyl pro-moieties targeting peptide transporters.
Steffansen
Bente
B
Molecular Biopharmaceutics, Department of Pharmaceutics, The Danish University of Pharmaceutical Sciences, Copenhagen, Denmark. bds@dfuni.dk
Nielsen
Carsten Uhd
CU
Frokjaer
Sven
S
D000818:Animals; D004151:Dipeptides / Q000378:metabolism; D016503:Drug Delivery Systems; D004355:Drug Stability; D006801:Humans; D007408:Intestinal Absorption; D026901:Membrane Transport Proteins / Q000502:physiology*; D010455:Peptides / Q000378:metabolism*; D011355:Prodrugs / Q000378:metabolism
D004151:Dipeptides; D026901:Membrane Transport Proteins; D010455:Peptides; D011355:Prodrugs; C043912:peptide permease