Structural characterization of the interaction of the polyene antibiotic Amphotericin B with DODAB bicelles and vesicles

摘要: Amphotericin B (AmB) is widely used in the treatment of systemic fungal infections, despite its toxic effects. Nephrotoxicity, ascribed as most serious effect, has been related to state aggregation antibiotic. In search increase AmB antifungal activity associated with low toxicity, several AmB-amphiphile formulations have proposed. This work focuses on structural characterization a specific formulation: sonicated dioctadecyl dimethylammonium bromide (DODAB) aggregates. Here, it was confirmed that DODAB dispersion constituted by bicelles, and monomeric much more soluble bicelles than vesicles. A new optical parameter proposed for estimation relative amount amphiphile-bound AmB. With theoretical simulations spectra spin labels incorporated possible prove binds preferentially lipids located at edges rigidifying them, decreasing polarity region. That special binding along borders where are highly disorganized, could be formulation other carriers antibiotic, including mixtures natural which known form bicelles.