BIBLIOS

Document type
Journal articles

Document subtype
Full paper

Title
Interactions of N′-acetyl-rifabutin and N′-butanoyl-rifabutin with lipid bilayers: A synchrotron X-ray study

Participants in the publication
Marina Pinheiro (Author)
Cláudia Nunes (Author)
João M. Caio (Author)
Cristina Moiteiro (Author)
Dep. Química e Bioquímica
Gerald Brezesinski (Author)
Salette Reis (Author)

Summary
This work focuses on the interaction of rifabutin (RFB), a naphthalenic ansamycin, with membrane models. Since the therapeutic and toxic effects of this class of drugs are strongly influenced by their lipid affinity, we concerned specifically on the ability of this antibiotic to affect the membrane biophysical properties. The extent of the interaction between RFB and membrane phospholipids was quantified by the partition coefficient (Kp), using membrane model systems that mimic the human (liposomes of 1,2-dimyristoyl-sn-glycero-phosphocholine, DMPC) and the bacterial (liposomes of 1,2-dimyristoyl-sn-glycero-3-phosphoglycerol, DMPG) plasma membranes. To predict the drug location in the membranes, fluorescence quenching and lifetime measurements were carried out using the above-mentioned membrane models labeled with fluorescent probes. Steady-state anisotropy measurements were also performed to evaluate the effect of RFB on the microviscosity of the membranes. Overall, the results support that RFB has higher affinity for the bacterial membrane mediated by electrostatic interactions with the phospholipid head groups.


Where published
International Journal of Pharmaceutics

Publication Identifiers
ISSN - 0378-5173

Publisher
Elsevier BV



Document Identifiers
DOI - https://doi.org/10.1016/j.ijpharm.2013.06.018
URL - http://dx.doi.org/10.1016/j.ijpharm.2013.06.018