Journal
BIOPHYSICAL CHEMISTRY
Volume 196, Issue -, Pages 92-99Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.bpc.2014.10.002
Keywords
Critical micelle concentration (CMC); BODIPY-alkylphosphocholine; Human leishmaniasis; Leishmanicidal drug
Funding
- FAPESP [09/54044-3, 2010/08652-9]
- CNPq [304981/2012-5]
- EU (from Fondo de Investigaciones Sanitarias, FIS, Ministerio de Sanidad y Consumo of Spain) [QlK2-CT-2001-01404, RD06/ 0021/0006, PI061125]
- Ministerio de Ciencia e Innovacion, Spain [CTQ2010-16457]
- Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [09/54044-3, 10/08652-9] Funding Source: FAPESP
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Miltefosine (hexadecylphosphocholine, MT) afforded successful oral treatment against human visceral and cutaneous leishmaniasis. Knowledge of MT aggregation in aqueous solutions and of its interaction with lipid membranes is important to understand pharmacokinetics, bioavailability and antiparasitic effects. Methods based on surface tension and fluorescence spectroscopy gave the value of 50 mu M for critical micelle concentration (CMC) in buffered water solution, and the value is influenced by salt content. Interaction between MT and lipid vesicles was monitored by fluorescence and the drug promotes only minor changes in the surface of the vesicles. At MT concentration below CMC, modifications in probe fluorescence are due to disordering effects promoted by the drug in the bilayer. Above the CMC, MT promoted large modifications in the vesicles as a whole, resulting in mixed aggregates containing lipids, drug and probe. Effects are less evident above thermal phase transition when the bilayer is in less ordered state. (C) 2014 Elsevier B.V. All rights reserved.
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