TY  - JOUR
AU  - Pereira-Leite, Catarina
AU  - Carneiro, Cláudia
AU  - Soares, José X.
AU  - Afonso, Carlos
AU  - Nunes, Cláudia
AU  - Lúcio, Marlene
AU  - Reis, Salette
TI  - Biophysical characterization of the drug–membrane interactions: The case of propranolol and acebutolol
JO  - European journal of pharmaceutics and biopharmaceutics
VL  - 84
IS  - 1
SN  - 0939-6411
CY  - New York, NY [u.a.]
PB  - Elsevier
M1  - DESY-2014-02141
SP  - 183 - 191
PY  - 2013
AB  - The interaction of propranolol and acebutolol with biological membranes was assessed in the present work by using a range of biophysical techniques and liposomes, as membrane mimetic models. Liposomes were made of zwitterionic phosphatidylcholines and experiments were performed at physiologic pH and at various membrane physical states (gel, ripple and fluid phases). Fluorescence techniques were used to study the partition coefficient of β-blockers, the influence of drugs on membrane fluidity and the drugs–membrane binding. Moreover, small and wide angle X-ray scattering techniques were used to evaluate the β-blockers effect on long range bilayer order and hydrocarbon chain packing. The gathered results highlighted the importance of electrostatic interactions between propranolol and acebutolol with membranes. Furthermore, both β-blockers exhibited a membrane-fluidizing effect and the capacity to disturb the membrane organization. In general, propranolol unveiled a more pronounced effect on membrane fluidity and structure than acebutolol. In the current study, the obtained results were also correlated with the cardioprotective properties of the β-blockers studied.
LB  - PUB:(DE-HGF)16
UR  - <Go to ISI:>//WOS:000319234600019
C6  - pmid:23291047
DO  - DOI:10.1016/j.ejpb.2012.12.005
UR  - https://bib-pubdb1.desy.de/record/167815
ER  -