Evaluating ternary systems with oligosaccharides as a strategy to improve the biopharmaceutical properties of furosemide

Mater Sci Eng C Mater Biol Appl. 2020 Jun:111:110793. doi: 10.1016/j.msec.2020.110793. Epub 2020 Feb 29.

Abstract

Novel ternary systems with β-cyclodextrin or maltodextrin and triethanolamine as the third component were developed with the aim of improving the oral bioavailability of furosemide. These new solids were characterized by solid-state nuclear magnetic resonance, Fourier transform infrared and Raman spectroscopy, X-ray powder diffractometry, scanning electron microscopy, thermogravimetric analysis, and differential scanning calorimetry. The solubility, dissolution and stability (chemical and physical) were studied. Among the most important results, it was observed that both ternary systems showed an important enhancement in the solubility of the drug. In particular, the system obtained by combination of β-cyclodextrin and TEA exhibited improvement in the dissolution profiles and photo-stability of furosemide compared with the binary system previously reported. Moreover, this system constitutes an interesting therapeutic alternative as it did not produce cellular toxicity compared with free furosemide. In conclusion, the results obtained revealed that this ternary system establishes a promising approach for oral delivery of the drug.

Keywords: Cellular toxicity; Dissolution; Furosemide; Oligosaccharides; Stability; Triethanolamine.

MeSH terms

  • Biological Products / pharmacology*
  • Calorimetry, Differential Scanning
  • Cell Death / drug effects
  • Furosemide / pharmacology*
  • HEK293 Cells
  • Humans
  • Magnetic Resonance Spectroscopy
  • Oligosaccharides / chemistry*
  • Powders
  • Solubility
  • Spectroscopy, Fourier Transform Infrared
  • Spectrum Analysis, Raman
  • Thermogravimetry
  • X-Ray Diffraction

Substances

  • Biological Products
  • Oligosaccharides
  • Powders
  • Furosemide