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.
Hayes
Patricia Y
PY
Discipline of Chemistry, School of Molecular and Microbial Sciences, and School of Pharmacy, The University of Queensland, Brisbane, Queensland 4072, Australia.
Ross
Benjamin P
BP
Thomas
Bradley G
BG
Toth
Istvan
I
D000284:Administration, Oral; D000818:Animals; D000925:Anticoagulants / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D002151:Calorimetry / Q000379:methods; D002412:Cations; D006495:Heparin, Low-Molecular-Weight / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D008055:Lipids / Q000008:administration & dosage*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D015394:Molecular Structure; D051381:Rats
D000925:Anticoagulants; D002412:Cations; D006495:Heparin, Low-Molecular-Weight; D008055:Lipids