The aqueous dissolution of a poorly soluble drug nystatin (Nys) was achieved by a simple, excipient-free procedure using a tromethamol-modified polysiloxane (ST) as surfactant. Long-term stable Nys aqueous formulation was prepared and investigated by different methods, in order to understand the mechanism of drug solubilization. The cryo-TEM analysis revealed the presence of soft vesicles in the Nyst_ST solution. According to TEM measurements, the drug is contained in the hydrophobic layer of the surfactant vesicles. The dynamic light scattering (DLS) measurements on Nys ST showed a main population around 134 nm having the Zeta potential of 33.3 mV. FT-IR, UV-vis, and thermogravimetric (TG-DTG-DTA) data point toward physical encapsulation, accompanied by a decrease of H-bonding between the drug molecules. The antifungal activity tested in vitro toward four yeast strains was seriously improved compared to the aqueous dispersion of the native drug, although the availability was diminished compared to DMSO solution. (C) 2013 Elsevier B.V. All rights reserved.
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Merck & Co Inc, Dept Oral Formulat Sci & Technol, West Point, PA 19486 USAMerck & Co Inc, Dept Oral Formulat Sci & Technol, West Point, PA 19486 USA
Sotthivirat, Sutthilug
Ramesh, Rishi
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Merck & Co Inc, Dept Pharmaceut Commercializat Technol, West Point, PA 19486 USAMerck & Co Inc, Dept Oral Formulat Sci & Technol, West Point, PA 19486 USA
Ramesh, Rishi
Wasylaschuk, Walter
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Merck & Co Inc, Dept Analyt Sci, West Point, PA 19486 USAMerck & Co Inc, Dept Oral Formulat Sci & Technol, West Point, PA 19486 USA
Wasylaschuk, Walter
Bottone, Cory
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Merck & Co Inc, Dept Analyt Sci, West Point, PA 19486 USAMerck & Co Inc, Dept Oral Formulat Sci & Technol, West Point, PA 19486 USA
Bottone, Cory
Xia, Binfeng
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Merck & Co Inc, Dept Biopharmaceut, West Point, PA 19486 USAMerck & Co Inc, Dept Oral Formulat Sci & Technol, West Point, PA 19486 USA
Xia, Binfeng
Stellabott, Joyce
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Merck & Co Inc, Dept Preformutat, West Point, PA 19486 USAMerck & Co Inc, Dept Oral Formulat Sci & Technol, West Point, PA 19486 USA
Stellabott, Joyce
McNevin, Michael
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Dept Mol & Mat Characterizat, West Point, PA USAMerck & Co Inc, Dept Oral Formulat Sci & Technol, West Point, PA 19486 USA
McNevin, Michael
Skomski, Daniel
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Merck & Co Inc, Dept Preformutat, West Point, PA 19486 USAMerck & Co Inc, Dept Oral Formulat Sci & Technol, West Point, PA 19486 USA
Skomski, Daniel
Brown, Chad
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Merck & Co Inc, Dept Oral Formulat Sci & Technol, West Point, PA 19486 USAMerck & Co Inc, Dept Oral Formulat Sci & Technol, West Point, PA 19486 USA