Galangin/β-Cyclodextrin Inclusion Complex as a Drug-Delivery System for Improved Solubility and Biocompatibility in Breast Cancer Treatment
The purpose of this study was to evaluate the potential of a newly modified cyclodextrin derivative, water-soluble β-cyclodextrin–epichlorohydrin (β-CD), as an effective drug carrier to enhance the poor solubility and bioavailability of galangin (GAL), a poorly water-soluble model drug. In this rega...
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MDPI AG
2022-07-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/27/14/4521 |
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| author | Zainab S. Abbas Ghassan M. Sulaiman Majid S. Jabir Salman A. A. Mohammed Riaz A. Khan Hamdoon A. Mohammed Amal Al-Subaiyel |
| author_facet | Zainab S. Abbas Ghassan M. Sulaiman Majid S. Jabir Salman A. A. Mohammed Riaz A. Khan Hamdoon A. Mohammed Amal Al-Subaiyel |
| author_sort | Zainab S. Abbas |
| collection | DOAJ |
| description | The purpose of this study was to evaluate the potential of a newly modified cyclodextrin derivative, water-soluble β-cyclodextrin–epichlorohydrin (β-CD), as an effective drug carrier to enhance the poor solubility and bioavailability of galangin (GAL), a poorly water-soluble model drug. In this regard, inclusion complexes of GAL/β-CDP were prepared. UV-VIS spectrophotometry, Fourier-transform infrared spectroscopy (FTIR), X-ray crystallography (XRD), zeta potential analysis, particle size analysis, field emission scanning electron microscopy (FESEM), and transmission electron microscopy (TEM) were applied to characterize the synthesized GAL/β-CD. Michigan Cancer Foundation-7 (MCF-7; human breast cancer cells) and rat embryo fibroblast (REF; normal cells) were employed to examine the in vitro cytotoxic effects of GAL/β-CD using various parameters. The dye-based tests of MTT and crystal violet clearly exhibited that GAL/β-CD-treated cells had a reduced proliferation rate, an influence that was not found in the normal cell line. The cells’ death was found to follow apoptotic mechanisms, as revealed by the dye-based test of acridine orange/ethidium bromide (AO/EtBr), with the involvement of the mitochondria via caspase-3-mediated events, as manifested by the Rh 123 test. We also included a mouse model to examine possible in vivo toxic effects of GAL/β-CD. It appears that the inclusion complex does not have a significant influence on normal cells, as indicated by serum levels of kidney and liver enzymatic markers, as well as thymic and splenic mass indices. A similar conclusion was reached on the histological level, as manifested by the absence of pathological alterations in the liver, kidney, thymus, spleen, heart, and lung. |
| first_indexed | 2024-03-09T06:07:44Z |
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| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-09T06:07:44Z |
| publishDate | 2022-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-e28d036c58b04a26abe1dbbde8d3ac192023-12-03T12:01:48ZengMDPI AGMolecules1420-30492022-07-012714452110.3390/molecules27144521Galangin/β-Cyclodextrin Inclusion Complex as a Drug-Delivery System for Improved Solubility and Biocompatibility in Breast Cancer TreatmentZainab S. Abbas0Ghassan M. Sulaiman1Majid S. Jabir2Salman A. A. Mohammed3Riaz A. Khan4Hamdoon A. Mohammed5Amal Al-Subaiyel6Division of Biotechnology, Department of Applied Science, University of Technology, Baghdad 10066, IraqDivision of Biotechnology, Department of Applied Science, University of Technology, Baghdad 10066, IraqDivision of Biotechnology, Department of Applied Science, University of Technology, Baghdad 10066, IraqDepartment of Pharmacology and Toxicology, College of Pharmacy, Qassim University, Qassim 51452, Saudi ArabiaDepartment of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Qassim University, Qassim 51452, Saudi ArabiaDepartment of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Qassim University, Qassim 51452, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Qassim University, Qassim 51452, Saudi ArabiaThe purpose of this study was to evaluate the potential of a newly modified cyclodextrin derivative, water-soluble β-cyclodextrin–epichlorohydrin (β-CD), as an effective drug carrier to enhance the poor solubility and bioavailability of galangin (GAL), a poorly water-soluble model drug. In this regard, inclusion complexes of GAL/β-CDP were prepared. UV-VIS spectrophotometry, Fourier-transform infrared spectroscopy (FTIR), X-ray crystallography (XRD), zeta potential analysis, particle size analysis, field emission scanning electron microscopy (FESEM), and transmission electron microscopy (TEM) were applied to characterize the synthesized GAL/β-CD. Michigan Cancer Foundation-7 (MCF-7; human breast cancer cells) and rat embryo fibroblast (REF; normal cells) were employed to examine the in vitro cytotoxic effects of GAL/β-CD using various parameters. The dye-based tests of MTT and crystal violet clearly exhibited that GAL/β-CD-treated cells had a reduced proliferation rate, an influence that was not found in the normal cell line. The cells’ death was found to follow apoptotic mechanisms, as revealed by the dye-based test of acridine orange/ethidium bromide (AO/EtBr), with the involvement of the mitochondria via caspase-3-mediated events, as manifested by the Rh 123 test. We also included a mouse model to examine possible in vivo toxic effects of GAL/β-CD. It appears that the inclusion complex does not have a significant influence on normal cells, as indicated by serum levels of kidney and liver enzymatic markers, as well as thymic and splenic mass indices. A similar conclusion was reached on the histological level, as manifested by the absence of pathological alterations in the liver, kidney, thymus, spleen, heart, and lung.https://www.mdpi.com/1420-3049/27/14/4521galanginβ-cyclodextrindrug deliverybiocompatibilitycytotoxicitycaspase-3 pathway |
| spellingShingle | Zainab S. Abbas Ghassan M. Sulaiman Majid S. Jabir Salman A. A. Mohammed Riaz A. Khan Hamdoon A. Mohammed Amal Al-Subaiyel Galangin/β-Cyclodextrin Inclusion Complex as a Drug-Delivery System for Improved Solubility and Biocompatibility in Breast Cancer Treatment Molecules galangin β-cyclodextrin drug delivery biocompatibility cytotoxicity caspase-3 pathway |
| title | Galangin/β-Cyclodextrin Inclusion Complex as a Drug-Delivery System for Improved Solubility and Biocompatibility in Breast Cancer Treatment |
| title_full | Galangin/β-Cyclodextrin Inclusion Complex as a Drug-Delivery System for Improved Solubility and Biocompatibility in Breast Cancer Treatment |
| title_fullStr | Galangin/β-Cyclodextrin Inclusion Complex as a Drug-Delivery System for Improved Solubility and Biocompatibility in Breast Cancer Treatment |
| title_full_unstemmed | Galangin/β-Cyclodextrin Inclusion Complex as a Drug-Delivery System for Improved Solubility and Biocompatibility in Breast Cancer Treatment |
| title_short | Galangin/β-Cyclodextrin Inclusion Complex as a Drug-Delivery System for Improved Solubility and Biocompatibility in Breast Cancer Treatment |
| title_sort | galangin β cyclodextrin inclusion complex as a drug delivery system for improved solubility and biocompatibility in breast cancer treatment |
| topic | galangin β-cyclodextrin drug delivery biocompatibility cytotoxicity caspase-3 pathway |
| url | https://www.mdpi.com/1420-3049/27/14/4521 |
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