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Title: Physiological concentrations of albumin favor drug binding
Authors: Tatlıdil, Diğdem
Üçüncü, Muhammed
Akdoğan, Yaşar
Keywords: Bovine serum albumin
Salicylic acid
Electron Spin Resonance
Binding site
Issue Date: 29-Jun-2015
Publisher: Royal Society of Chemistry
Source: Tatlıdil, D., Üçüncü, M., and Akdoğan, Y. (2015). Physiological concentrations of albumin favor drug binding. Physical Chemistry Chemical Physics, 17(35), 22678-22685. doi:10.1039/c5cp03583j
Abstract: The ability to track drug binding and release makes electron paramagnetic resonance (EPR) spectroscopy well suited for drug delivery studies. Using the continuous wave (cw) EPR technique to extract information about the dynamics of the spin labeled drugs we can simultaneously determine the bound and unbound drugs. Here, spin labeled salicylic acid (SLSA) binding to and release from bovine serum albumin (BSA) is investigated, as a model for drug-transport protein interaction. We studied SLSA-BSA binding in a wide concentration range and found that the stoichiometry of the drug-protein increases significantly when the physiological range of BSA concentration is reached. Our EPR results explicitly reveal that up to ∼7 SLSA can bind to one albumin at the physiological concentration, whereas at lower BSA concentrations (<0.125 mM) the SLSA-BSA stoichiometry is maximum 2. Moreover, we studied drug release and showed that the ratio of bound to unbound SLSA concentrations remains relatively stable during dialysis. This indicates that the binding equilibrium of SLSA is not altered through the process of dialysis. This study demonstrates that cw EPR spectroscopy in combination with spin labeled drugs is an effective technique for binding and release studies and stoichiometric analysis of drug-protein interactions.
ISSN: 1463-9076
Appears in Collections:Chemistry / Kimya
Materials Science and Engineering / Malzeme Bilimi ve Mühendisliği
PubMed İndeksli Yayınlar Koleksiyonu / PubMed Indexed Publications Collection
Scopus İndeksli Yayınlar Koleksiyonu / Scopus Indexed Publications Collection
WoS İndeksli Yayınlar Koleksiyonu / WoS Indexed Publications Collection

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