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Physicochemical Characterization, Molecular Docking, and In Vitro Dissolution of Glimepiride–Captisol Inclusion Complexes
[Image: see text] This present study investigated the effect of Captisol, a chemically modified cyclodextrin, on the in vitro dissolution of glimepiride. We prepared glimepiride–Captisol complexes of different mass ratios (1:1, 1:2, and 1:3 w/w) by a physical mixing or freeze-drying technique, and f...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical Society
2020
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7439272/ https://www.ncbi.nlm.nih.gov/pubmed/32832751 http://dx.doi.org/10.1021/acsomega.0c01228 |
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author | Pal, Arpita Roy, Sudeep Kumar, Akhil Mahmood, Syed Khodapanah, Nasrin Thomas, Sabu Agatemor, Christian Ghosal, Kajal |
author_facet | Pal, Arpita Roy, Sudeep Kumar, Akhil Mahmood, Syed Khodapanah, Nasrin Thomas, Sabu Agatemor, Christian Ghosal, Kajal |
author_sort | Pal, Arpita |
collection | PubMed |
description | [Image: see text] This present study investigated the effect of Captisol, a chemically modified cyclodextrin, on the in vitro dissolution of glimepiride. We prepared glimepiride–Captisol complexes of different mass ratios (1:1, 1:2, and 1:3 w/w) by a physical mixing or freeze-drying technique, and found that complexation with Captisol enhanced the water solubility of glimepiride. Molecular docking and dynamic simulation predicted complex formation; at the same time, Fourier transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffractometry, and scanning electron microscope indicated molecular interactions that support complexation. We also found that an inclusion complex was better than a physical mixture in enhancing the complexation of glimepiride with Captisol and enhancing water solubility. Phase solubility study of the glimepiride–Captisol complex showed an A(L)-type profile, implying the formation of a 1:1 inclusion complex. The study also revealed that pH influenced the stability of the complex because the stability constant of the glimepiride–Captisol complex was higher in distilled water of pH ∼6.0 than in phosphate buffer of pH 7.2. |
format | Online Article Text |
id | pubmed-7439272 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | American Chemical Society |
record_format | MEDLINE/PubMed |
spelling | pubmed-74392722020-08-21 Physicochemical Characterization, Molecular Docking, and In Vitro Dissolution of Glimepiride–Captisol Inclusion Complexes Pal, Arpita Roy, Sudeep Kumar, Akhil Mahmood, Syed Khodapanah, Nasrin Thomas, Sabu Agatemor, Christian Ghosal, Kajal ACS Omega [Image: see text] This present study investigated the effect of Captisol, a chemically modified cyclodextrin, on the in vitro dissolution of glimepiride. We prepared glimepiride–Captisol complexes of different mass ratios (1:1, 1:2, and 1:3 w/w) by a physical mixing or freeze-drying technique, and found that complexation with Captisol enhanced the water solubility of glimepiride. Molecular docking and dynamic simulation predicted complex formation; at the same time, Fourier transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffractometry, and scanning electron microscope indicated molecular interactions that support complexation. We also found that an inclusion complex was better than a physical mixture in enhancing the complexation of glimepiride with Captisol and enhancing water solubility. Phase solubility study of the glimepiride–Captisol complex showed an A(L)-type profile, implying the formation of a 1:1 inclusion complex. The study also revealed that pH influenced the stability of the complex because the stability constant of the glimepiride–Captisol complex was higher in distilled water of pH ∼6.0 than in phosphate buffer of pH 7.2. American Chemical Society 2020-08-04 /pmc/articles/PMC7439272/ /pubmed/32832751 http://dx.doi.org/10.1021/acsomega.0c01228 Text en Copyright © 2020 American Chemical Society This is an open access article published under an ACS AuthorChoice License (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes. |
spellingShingle | Pal, Arpita Roy, Sudeep Kumar, Akhil Mahmood, Syed Khodapanah, Nasrin Thomas, Sabu Agatemor, Christian Ghosal, Kajal Physicochemical Characterization, Molecular Docking, and In Vitro Dissolution of Glimepiride–Captisol Inclusion Complexes |
title | Physicochemical Characterization, Molecular Docking,
and In Vitro Dissolution of Glimepiride–Captisol
Inclusion Complexes |
title_full | Physicochemical Characterization, Molecular Docking,
and In Vitro Dissolution of Glimepiride–Captisol
Inclusion Complexes |
title_fullStr | Physicochemical Characterization, Molecular Docking,
and In Vitro Dissolution of Glimepiride–Captisol
Inclusion Complexes |
title_full_unstemmed | Physicochemical Characterization, Molecular Docking,
and In Vitro Dissolution of Glimepiride–Captisol
Inclusion Complexes |
title_short | Physicochemical Characterization, Molecular Docking,
and In Vitro Dissolution of Glimepiride–Captisol
Inclusion Complexes |
title_sort | physicochemical characterization, molecular docking,
and in vitro dissolution of glimepiride–captisol
inclusion complexes |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7439272/ https://www.ncbi.nlm.nih.gov/pubmed/32832751 http://dx.doi.org/10.1021/acsomega.0c01228 |
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