Journal
MOLECULES
Volume 27, Issue 17, Pages -Publisher
MDPI
DOI: 10.3390/molecules27175600
Keywords
disulfiram; solubility; beta-cyclodextrin; SARS-CoV-19; nebulization
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This study aimed to improve the solubility of Disulfiram (DS) by forming inclusion complexes with cyclodextrins (CDs). The results showed that the CD inclusion complexes significantly increased the aqueous solubility of DS and exhibited suitable aerosolization properties. The CD inclusion complexes have great potential for enhancing the solubility of DS.
Disulfiram (DS), known as an anti-alcoholism drug, has shown a potent antiviral activity. Still, the potential clinical application of DS is limited by its low water solubility and rapid metabolism. Cyclodextrins (CDs) have been widely used to improve the solubility of drugs in water. In this study, five concentrations of hydroxypropyl beta-cyclodextrin (HP) and sulfobutyl ether beta-cyclodextrin (SBE) were used to form inclusion complexes of DS for enhanced solubility. Solutions were freeze-dried, and the interaction between DS and CD was characterized using differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), and Fourier transform infrared spectroscopy (FTIR). In addition, the nebulization properties of the DS-CD solutions were studied. The aqueous solubility of DS increased significantly when loaded to either of both CDs. The phase solubility of both complexes was a linear function of the CD concentration (A(L) type). Furthermore, physicochemical characterization studies showed a potent inclusion of the drug in the CD-DS complexes. Aerosolization studies demonstrated that these formulations are suitable for inhalation. Overall, the CD inclusion complexes have great potential for the enhancement of DS solubility. However, further studies are needed to assess the efficacy of DS-CD inclusion complexes against SARS-CoV-2 via nebulization.
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