A polysiloxane surfactant dissolves a poorly soluble drug (nystatin) in water

作者：Racles Carmen^*; Mares Mihai; Sacarescu Liviu

来源：Colloids and Surfaces A: Physicochemical and Engineering Aspects , 2014, 443: 233-239.

DOI：10.1016/j.colsurfa.2013.11.010

• Surfactant
• Nystatin
• Dissolution
• Polysiloxane
• Vesicles
• Antifungal activity

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.

• 出版日期2014-2-20