Polycationic lipophilic-core dendrons as penetration enhancers for the oral administration of low molecular weight heparin

Two polycationic lipophilic-core carbohydrate-based dendrons 2a–b and five polycationic lipophilic-core peptide dendrons 3–6, containing four arginine or lysine terminal residues, were synthesized and then tested in rats as penetration enhancers for the oral delivery of low molecular weight heparin. Better results were obtained with dendrons containing terminal lysine residues than terminal arginine. A significant anti-factor Xa activity was obtained when low molecular weight heparin was coadministered with dendron 5.

Polycationic lipophilic-core dendrons were tested in rats as penetration enhancers for the oral delivery of low molecular weight heparin (LMWH). A significant anti-factor Xa activity was obtained when LMWH was coadministered with dendron 5.Figure optionsDownload as PowerPoint slide