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Published on: July 12, 2013
Articaine interaction with DSPC bilayer: a 13C and 31P solid-state NMR study
Chen Song1, Henning Lygre, Willy Nerdal
1Department of Chemistry, University of Bergen, Allégaten 41, N-5007 Bergen, Norway. Chen.Song@kj.uib.no
Articaine hydrochloride, a dental local anesthetic, significantly alters model membranes. Higher concentrations may lead to articaine aggregation within the distearoylphosphatidylcholine bilayer.
Area of Science:
- Pharmacology
- Biophysics
- Materials Science
Background:
- Articaine hydrochloride is an amide local anesthetic widely used in dentistry.
- Understanding its interaction with biological membranes is crucial for drug efficacy and safety.
Purpose of the Study:
- To investigate the interaction between uncharged articaine and distearoylphosphatidylcholine (DSPC) model membranes.
- To determine the effect of varying articaine concentrations on DSPC bilayer structure and dynamics.
Main Methods:
- Solid-state (13)C and (31)P Nuclear Magnetic Resonance (NMR) spectroscopy.
- Study of DSPC model membranes with articaine at 10, 25, 40, and 55 mol%.
Main Results:
- Articaine concentration-dependently decreased the DSPC bilayer's gel-to-liquid-crystalline phase-transition temperature.
- At 40 mol% articaine, NMR spectra indicated disturbed molecular packing in both polar and hydrophobic regions of the DSPC bilayer.
- Increasing articaine to 55 mol% suggested the formation of articaine aggregates and reduced bilayer perturbation.
Conclusions:
- Articaine interacts substantially with DSPC model membranes, affecting bilayer fluidity and structure.
- High concentrations of articaine may lead to self-aggregation, altering its membrane interaction profile.
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