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

Patricia Y Hayes; Benjamin P Ross; Bradley G Thomas; Istvan Toth

doi:10.1016/j.bmc.2005.08.004

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

Bioorg Med Chem. 2006 Jan 1;14(1):143-52. doi: 10.1016/j.bmc.2005.08.004. Epub 2005 Sep 16.

Authors

Patricia Y Hayes¹, Benjamin P Ross, Bradley G Thomas, Istvan Toth

Affiliation

¹ Discipline of Chemistry, School of Molecular and Microbial Sciences, and School of Pharmacy, The University of Queensland, Brisbane, Queensland 4072, Australia.

PMID: 16169233
DOI: 10.1016/j.bmc.2005.08.004

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Administration, Oral
Animals
Anticoagulants / administration & dosage*
Anticoagulants / chemistry
Anticoagulants / pharmacokinetics
Calorimetry / methods
Cations
Heparin, Low-Molecular-Weight / administration & dosage*
Heparin, Low-Molecular-Weight / chemistry
Heparin, Low-Molecular-Weight / pharmacokinetics
Lipids / administration & dosage*
Magnetic Resonance Spectroscopy
Mass Spectrometry
Molecular Structure
Rats

Substances

Anticoagulants
Cations
Heparin, Low-Molecular-Weight
Lipids