Insulin-cell penetrating peptide hybrids with improved intestinal absorption efficiency.
Cell-penetrating peptide (CPP) was linked to insulin to form insulin-CPP hybrids. The intestinal absorption efficiency of CPP hybridized insulin was 6-8 times increased compared to normal insulin as tested on Caco-2 cell monolayer, a widely used in vitro model for intestinal absorption. Insulin-CPP hybrid transportation seemed to be through an active and transcytosis-like mechanism. Importantly, insulin in hybrids kept intact after they passed through the Caco-2 cell monolayer. This study provides a new clue for oral insulin development.
Liang
Jun F
JF
Department of Chemistry and Chemical Biology, Stevens Institute of Technology, Hoboken, NJ 07030, USA. jliang2@stevens.edu
Yang
Victor C
VC
D000284:Administration, Oral; D000595:Amino Acid Sequence; D018938:Caco-2 Cells; D006801:Humans; D007328:Insulin / Q000737:chemistry / Q000378:metabolism* / Q000493:pharmacokinetics; D007408:Intestinal Absorption; D008969:Molecular Sequence Data; D010455:Peptides / Q000737:chemistry / Q000378:metabolism*
D007328:Insulin; D010455:Peptides