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CC BY-NC-ND 4.0 · International Journal of Epilepsy 2017; 04(02): 150-158
DOI: 10.1016/j.ijep.2017.09.001
Research paper
Thieme Medical and Scientific Publishers Private Ltd.

Divergent interaction profiles of gabapentin and levetiracetam with dipalmitoylphosphatidylcholine lipids

Sevgi Türker-Kaya
1   Kocaeli University, Faculty of Arts and Sciences, Department of Biology, 41380, Kocaeli, Turkey
,
Aygül Kına
1   Kocaeli University, Faculty of Arts and Sciences, Department of Biology, 41380, Kocaeli, Turkey
,
Selen Alın
1   Kocaeli University, Faculty of Arts and Sciences, Department of Biology, 41380, Kocaeli, Turkey
› Institutsangaben
Weitere Informationen

Publikationsverlauf

Received: 31. Januar 2017

Accepted: 13. September 2017

Publikationsdatum:
06. Mai 2018 (online)

   Lizenzen und Reprints

Abstract

Background/Objectives The lipid solubility of antiepileptic drugs directly affects central nervous system availability. In relation to this, the interactions of gabapentin and levetiracetam with dipalmitoylphosphatidylcholine lipids depending on concentrations were comparatively investigated in the present study.

Methods The effects of gabapentin and levetricetam as a function of concentration (1–5–10–20 mol%) on biophysical parameters of dipalmitoylphosphatidylcholine multilammelar vesicles were studied by differential scanning calorimetry and fourier transform infrared spectroscopy.

Results The data revealed that gabapentin at all concentrations and levetiracetam at 1–5 mol% lowered main transition temperature, enthalpy, cooperativity, lipid fluidity, lipid order, and increased hydrogen binding capacity of glycerol and phosphate groups. However, 10–20 mol% of levetiracetam tend to show different effect on transition temperature, which could also reflect its opposing effect on lipid order and glycerol and phosphate group’s hydrations.

Conclusions According to the corresponding findings depending on concentrations both drugs incorporate into phosphatidylcholines, perturbing the packing of lipids and affecting their thermotropic properties. Their binding affinity to acyl chains and hydrophilic parts of lipids was found to highly correlate with lipid-water partition and their solubility degree in water. Hence, the obtained results may offer evaluation of partition profile of the drugs into biological membranes depending on concentration.

Keywords

Gabapentin - Levetiracetam - Dipalmitoylphosphatidylcholines - Fourier transform infrared spectroscopy - Differential scanning calorimetry
 

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