Biophysical characterization of the drug-membrane interactions: The case of propranolol and acebutolol

• Type: Article in International Scientific Journal
• Date: 2013

Authors

Catarina Pereira Leite (Author) Other; Claudia Carneiro (Author) Other; Jose X Soares (Author) FFUP; Carlos Afonso (Author) FFUP; Claudia Nunes (Author) Other; Marlene Lucio (Author) FFUP; Salette Reis (Author) FFUP

Journal

Title: European Journal of Pharmaceutics and Biopharmaceutics

Vol. 84

Pages: 183-191

ISSN: 0939-6411

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 21 Citations

Scopus - 24 Citations

Scientific classification

FOS: Medical and Health sciences > Basic medicine

Other information

Authenticus ID: P-005-0YM

DOI: 10.1016/j.ejpb.2012.12.005

Abstract (EN): 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 beta-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 beta-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 beta-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 beta-blockers studied.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 9