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Formulation of Genistein-HP β Cyclodextrin-Poloxamer 188 Ternary Inclusion Complex: Solubility to Cytotoxicity Assessment
The current study was designed to prepare the inclusion complex Genistein (GS) using Hydroxypropyl β cyclodextrin (HP β CD) and poloxamer 188 (PL 188). The binary inclusion complex (GS BC) and ternary inclusion complex (GS TC) were developed by microwave irradiation technique and evaluated for a com...
Autores principales: | , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8707042/ https://www.ncbi.nlm.nih.gov/pubmed/34959278 http://dx.doi.org/10.3390/pharmaceutics13121997 |
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author | Zafar, Ameeduzzafar Alruwaili, Nabil K. Imam, Syed Sarim Alsaidan, Omar Awad Alkholifi, Faisal K. Alharbi, Khalid Saad Mostafa, Ehab M. Alanazi, Abdullah S. Gilani, Sadaf Jamal Musa, Arafa Alshehri, Sultan Rawaf, Alenazy Alquraini, Ali |
author_facet | Zafar, Ameeduzzafar Alruwaili, Nabil K. Imam, Syed Sarim Alsaidan, Omar Awad Alkholifi, Faisal K. Alharbi, Khalid Saad Mostafa, Ehab M. Alanazi, Abdullah S. Gilani, Sadaf Jamal Musa, Arafa Alshehri, Sultan Rawaf, Alenazy Alquraini, Ali |
author_sort | Zafar, Ameeduzzafar |
collection | PubMed |
description | The current study was designed to prepare the inclusion complex Genistein (GS) using Hydroxypropyl β cyclodextrin (HP β CD) and poloxamer 188 (PL 188). The binary inclusion complex (GS BC) and ternary inclusion complex (GS TC) were developed by microwave irradiation technique and evaluated for a comparative dissolution study. Further, the samples were assessed for FTIR, DSC, XRD, and NMR for the confirmation of complex formation. Finally, antioxidant and antimicrobial studies and cytotoxicity studies on a breast cancer (MCF-7) cell line were conducted. The dissolution study result showed a marked increment in GS dissolution/release after incorporation in binary (GS: HP β CD, 1:1) and ternary (GS: HP β CD: PL 188; 1:1:0.5) inclusion complexes. Moreover, the ternary complex exhibited a significant enhancement (p < 0.05) in dissolution than did the binary complexes. This might be due to the presence of PL 188, which helps in solubility enhancement of GS. DSC, XRD and SEM evaluation confirmed the modification in the structure of GS. FTIR and NMR results indicated the formation of an inclusion complex. The antioxidant and antimicrobial activity results revealed that GS TC has shown significant (p < 0.05) higher activity than pure GS. The cytotoxicity study results also depicted concentration-dependent cytotoxicity. GS TC exhibited significantly (p < 0.05) high cytotoxicity to cancer cells (IC(50) = 225 µg/mL) than pure GS (IC(50) = 480 µg/mL). Finally, it was concluded that a remarkable enhancement in the dissolution was observed after the inclusion of GS in the ternary complex and it therefore has significant potential for the treatment of breast cancer. |
format | Online Article Text |
id | pubmed-8707042 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-87070422021-12-25 Formulation of Genistein-HP β Cyclodextrin-Poloxamer 188 Ternary Inclusion Complex: Solubility to Cytotoxicity Assessment Zafar, Ameeduzzafar Alruwaili, Nabil K. Imam, Syed Sarim Alsaidan, Omar Awad Alkholifi, Faisal K. Alharbi, Khalid Saad Mostafa, Ehab M. Alanazi, Abdullah S. Gilani, Sadaf Jamal Musa, Arafa Alshehri, Sultan Rawaf, Alenazy Alquraini, Ali Pharmaceutics Article The current study was designed to prepare the inclusion complex Genistein (GS) using Hydroxypropyl β cyclodextrin (HP β CD) and poloxamer 188 (PL 188). The binary inclusion complex (GS BC) and ternary inclusion complex (GS TC) were developed by microwave irradiation technique and evaluated for a comparative dissolution study. Further, the samples were assessed for FTIR, DSC, XRD, and NMR for the confirmation of complex formation. Finally, antioxidant and antimicrobial studies and cytotoxicity studies on a breast cancer (MCF-7) cell line were conducted. The dissolution study result showed a marked increment in GS dissolution/release after incorporation in binary (GS: HP β CD, 1:1) and ternary (GS: HP β CD: PL 188; 1:1:0.5) inclusion complexes. Moreover, the ternary complex exhibited a significant enhancement (p < 0.05) in dissolution than did the binary complexes. This might be due to the presence of PL 188, which helps in solubility enhancement of GS. DSC, XRD and SEM evaluation confirmed the modification in the structure of GS. FTIR and NMR results indicated the formation of an inclusion complex. The antioxidant and antimicrobial activity results revealed that GS TC has shown significant (p < 0.05) higher activity than pure GS. The cytotoxicity study results also depicted concentration-dependent cytotoxicity. GS TC exhibited significantly (p < 0.05) high cytotoxicity to cancer cells (IC(50) = 225 µg/mL) than pure GS (IC(50) = 480 µg/mL). Finally, it was concluded that a remarkable enhancement in the dissolution was observed after the inclusion of GS in the ternary complex and it therefore has significant potential for the treatment of breast cancer. MDPI 2021-11-24 /pmc/articles/PMC8707042/ /pubmed/34959278 http://dx.doi.org/10.3390/pharmaceutics13121997 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Zafar, Ameeduzzafar Alruwaili, Nabil K. Imam, Syed Sarim Alsaidan, Omar Awad Alkholifi, Faisal K. Alharbi, Khalid Saad Mostafa, Ehab M. Alanazi, Abdullah S. Gilani, Sadaf Jamal Musa, Arafa Alshehri, Sultan Rawaf, Alenazy Alquraini, Ali Formulation of Genistein-HP β Cyclodextrin-Poloxamer 188 Ternary Inclusion Complex: Solubility to Cytotoxicity Assessment |
title | Formulation of Genistein-HP β Cyclodextrin-Poloxamer 188 Ternary Inclusion Complex: Solubility to Cytotoxicity Assessment |
title_full | Formulation of Genistein-HP β Cyclodextrin-Poloxamer 188 Ternary Inclusion Complex: Solubility to Cytotoxicity Assessment |
title_fullStr | Formulation of Genistein-HP β Cyclodextrin-Poloxamer 188 Ternary Inclusion Complex: Solubility to Cytotoxicity Assessment |
title_full_unstemmed | Formulation of Genistein-HP β Cyclodextrin-Poloxamer 188 Ternary Inclusion Complex: Solubility to Cytotoxicity Assessment |
title_short | Formulation of Genistein-HP β Cyclodextrin-Poloxamer 188 Ternary Inclusion Complex: Solubility to Cytotoxicity Assessment |
title_sort | formulation of genistein-hp β cyclodextrin-poloxamer 188 ternary inclusion complex: solubility to cytotoxicity assessment |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8707042/ https://www.ncbi.nlm.nih.gov/pubmed/34959278 http://dx.doi.org/10.3390/pharmaceutics13121997 |
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