Preparation and Characterization of Disulfiram and Beta Cyclodextrin Inclusion Complexes for Potential Application in the Treatment of SARS-CoV-2 via Nebulization
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,...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-08-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/27/17/5600 |
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| author | Ana Maria Pereira Ayse Kaya Dan Alves Niusha Ansari-Fard Ibrahim Tolaymat Basel Arafat Mohammad Najlah |
| author_facet | Ana Maria Pereira Ayse Kaya Dan Alves Niusha Ansari-Fard Ibrahim Tolaymat Basel Arafat Mohammad Najlah |
| author_sort | Ana Maria Pereira |
| collection | DOAJ |
| description | 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 β-cyclodextrin (HP) and sulfobutyl ether β-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<sub>L</sub> 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. |
| first_indexed | 2024-03-10T01:29:50Z |
| format | Article |
| id | doaj.art-8b8272d135004c14b1e03e2f1d784a76 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T01:29:50Z |
| publishDate | 2022-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-8b8272d135004c14b1e03e2f1d784a762023-11-23T13:44:55ZengMDPI AGMolecules1420-30492022-08-012717560010.3390/molecules27175600Preparation and Characterization of Disulfiram and Beta Cyclodextrin Inclusion Complexes for Potential Application in the Treatment of SARS-CoV-2 via NebulizationAna Maria Pereira0Ayse Kaya1Dan Alves2Niusha Ansari-Fard3Ibrahim Tolaymat4Basel Arafat5Mohammad Najlah6Pharmaceutical Research Group, School of Allied Health, Faculty of Health, Education, Medicine and Social Care, Anglia Ruskin University, Bishops Hall Lane, Chelmsford CM1 1SQ, UKPharmaceutical Research Group, School of Allied Health, Faculty of Health, Education, Medicine and Social Care, Anglia Ruskin University, Bishops Hall Lane, Chelmsford CM1 1SQ, UKPharmaceutical Research Group, School of Allied Health, Faculty of Health, Education, Medicine and Social Care, Anglia Ruskin University, Bishops Hall Lane, Chelmsford CM1 1SQ, UKPharmaceutical Research Group, School of Allied Health, Faculty of Health, Education, Medicine and Social Care, Anglia Ruskin University, Bishops Hall Lane, Chelmsford CM1 1SQ, UKPharmaceutical Research Group, School of Allied Health, Faculty of Health, Education, Medicine and Social Care, Anglia Ruskin University, Bishops Hall Lane, Chelmsford CM1 1SQ, UKPharmaceutical Research Group, School of Allied Health, Faculty of Health, Education, Medicine and Social Care, Anglia Ruskin University, Bishops Hall Lane, Chelmsford CM1 1SQ, UKPharmaceutical Research Group, School of Allied Health, Faculty of Health, Education, Medicine and Social Care, Anglia Ruskin University, Bishops Hall Lane, Chelmsford CM1 1SQ, UKDisulfiram (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 β-cyclodextrin (HP) and sulfobutyl ether β-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<sub>L</sub> 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.https://www.mdpi.com/1420-3049/27/17/5600disulfiramsolubilityβ-cyclodextrinSARS-CoV-19nebulization |
| spellingShingle | Ana Maria Pereira Ayse Kaya Dan Alves Niusha Ansari-Fard Ibrahim Tolaymat Basel Arafat Mohammad Najlah Preparation and Characterization of Disulfiram and Beta Cyclodextrin Inclusion Complexes for Potential Application in the Treatment of SARS-CoV-2 via Nebulization Molecules disulfiram solubility β-cyclodextrin SARS-CoV-19 nebulization |
| title | Preparation and Characterization of Disulfiram and Beta Cyclodextrin Inclusion Complexes for Potential Application in the Treatment of SARS-CoV-2 via Nebulization |
| title_full | Preparation and Characterization of Disulfiram and Beta Cyclodextrin Inclusion Complexes for Potential Application in the Treatment of SARS-CoV-2 via Nebulization |
| title_fullStr | Preparation and Characterization of Disulfiram and Beta Cyclodextrin Inclusion Complexes for Potential Application in the Treatment of SARS-CoV-2 via Nebulization |
| title_full_unstemmed | Preparation and Characterization of Disulfiram and Beta Cyclodextrin Inclusion Complexes for Potential Application in the Treatment of SARS-CoV-2 via Nebulization |
| title_short | Preparation and Characterization of Disulfiram and Beta Cyclodextrin Inclusion Complexes for Potential Application in the Treatment of SARS-CoV-2 via Nebulization |
| title_sort | preparation and characterization of disulfiram and beta cyclodextrin inclusion complexes for potential application in the treatment of sars cov 2 via nebulization |
| topic | disulfiram solubility β-cyclodextrin SARS-CoV-19 nebulization |
| url | https://www.mdpi.com/1420-3049/27/17/5600 |
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