ABSTRACT
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 50µM 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.
Subject(s)
Antiparasitic Agents/chemistry , Boron Compounds/chemistry , Phosphorylcholine/analogs & derivatives , Phosphorylcholine/chemistry , Antiparasitic Agents/metabolism , Azoles/chemistry , Humans , Nitrobenzenes/chemistry , Phosphorylcholine/metabolism , Spectrometry, Fluorescence , Surface Tension , Unilamellar Liposomes/chemistry , Unilamellar Liposomes/metabolismABSTRACT
The photothermal properties and heat diffusion of polymeric lasers, made up from solutions of Rhodamine 6G in solid matrices of poly(2-hydroxyethyl methacrylate) with different amounts of the cross-linking monomer ethylene glycol dimethacrylate and copolymers of 2-hydroxyethyl methacrylate and methyl methacrylate have been studied through photothermal deflection spectroscopy. The heat load that is due to the pumping process was quantified as a function of the pump excitation repetition frequency (0.25-10 Hz), determining the time-dependent temperature changes at different locations within the laser matrix. A theoretical model, which reproduces these changes with high accuracy, was developed on the basis of the heat-diffusion equation of optically dense fluids. The observed thermal effects became important for impairing the laser stability at pump repetition frequencies higher than 1 Hz. In addition, the irreversible optical changes produced in the laser matrices at high pump fluence values (>1 J/cm2) were also analyzed. These effects originate, most likely, from a two-step photothermal mechanism.
