Interaction of rifabutin with model membranes

Abstract

Liposomal and free rifabutin were separated by the method of gel filtration. The percents of rifabutin bound to liposomes of different phospholipid composition were measured. The presence of negatively charged phospholipids increased the degree of binding. Binding decreased with increasing the ionic strength. Incubation of rifabutin with liposomes containing anthryl phosphatidylcholine was accompanied by fluorescence quenching. Activity of rifabutin depended on the phospholipid composition of liposomes. Our results indicate that binding of rifabutin is associated with electrostatic and hydrophobic interactions.

Molecular Interaction of Rifabutin on Model Lung Surfactant Monolayers

“…Previous studies deal with the interactions of RBT with 3D models, such as multilamellar and unilamellar phospholipid vesicles. 9,10 However, the first steps in the interaction of RBT with the components of the lung surfactants occur at the monolayer/drug interface.…”

“…Literature is particularly poor in information related to drugs accessibility and interaction with the lipid content of this barrier. Previous studies deal with the interactions of RBT with 3D models, such as multilamellar and unilamellar phospholipid vesicles. , However, the first steps in the interaction of RBT with the components of the lung surfactants occur at the monolayer/drug interface.…”

Differential Interactions of Rifabutin with Human and Bacterial Membranes: Implication for Its Therapeutic and Toxic Effects

“…Previous works reported the higher preference of RFB for negatively charged membrane models. 11,12,17 Vostrikov and co-workers 12 determined the distribution coefficient of RFB by fluorescence quenching using LUVs of PC and PC:cardiolipin (CL) and concluded that RFB might establish electrostatic interactions with the membranes due to the higher distribution obtained in the negatively charged model. Using phase separation and fluorescence quenching, Vostrikov and colleagues determined the distribution coefficient of RFB and proved that the insertion of a CL in PC multilamellar liposomes (MLVs) increases the binding of RFB to the lipid bilayer.…”