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Interactions of amidated acids with heparin
Ruel Z B Desamero1, Hu Cheng, Sean Cahill
1Department of Physics, City College of New York, New York, New York 10031, USA.
Biopolymers
|February 14, 2002
Summary
Heparin oral delivery agents, amidated acids, form complexes with heparin near its OH groups. Protonation of the agent's carboxyl groups may enhance oral heparin absorption.
Area of Science:
- Biochemistry
- Drug Delivery
- Materials Science
Background:
- Heparin is crucial for anticoagulation but requires parenteral administration.
- Oral heparin delivery faces challenges due to poor gastrointestinal absorption.
- Amidated acids are investigated as potential delivery agents to improve oral heparin bioavailability.
Purpose of the Study:
- To characterize the solution structures of complexes formed between heparin and amidated acids.
- To elucidate the interaction mechanisms between heparin and these delivery agents.
- To identify structural features contributing to the efficacy of oral heparin delivery.
Main Methods:
- Raman spectroscopy was employed to study molecular vibrations and interactions.
- Nuclear Magnetic Resonance (NMR) spectroscopy was used to determine solution structures and binding sites.
- Complexation studies were performed at concentrations relevant to oral drug delivery.
Main Results:
- Complexation occurs near the hydroxyl (OH) groups of heparin.
- Heparin exhibits non-specific interactions with both monomeric and self-associated amidated acids.
- Carboxyl groups of the delivery agents readily protonate upon complexation with heparin or self-association.
Conclusions:
- The non-specific interaction and protonation of amidated acids are key factors in facilitating heparin's oral absorption.
- These findings provide insights into the design of effective oral heparin delivery systems.
- The study highlights the potential of amidated acids as carriers for enhancing the oral bioavailability of heparin.