Hybrid nanoparticulate system of Fluvastatin loaded phospholipid, alpha lipoic acid and melittin for the management of colon cancer
As a hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, Fluvastatin (FLV) is used for reducing low-density lipoprotein (LDL) cholesterol as well as to prevent cardiovascular problems. FLV showed cell line cytotoxicity and antitumor effect. Melittin (MEL) exhibits antineoplastic activity...
| Main Authors: | , , , , , |
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| Format: | Article |
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Nature Publishing Group
2022
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| Online Access: | http://psasir.upm.edu.my/id/eprint/101752/ |
| _version_ | 1848863623546404864 |
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| author | Alfaleh, Mohamed A. Fahmy, Omar Abourehab, Mohammed A. S. Fahmy, Usama A. Alharbi, Awaad S. Alhakamy, Nabil A. |
| author_facet | Alfaleh, Mohamed A. Fahmy, Omar Abourehab, Mohammed A. S. Fahmy, Usama A. Alharbi, Awaad S. Alhakamy, Nabil A. |
| author_sort | Alfaleh, Mohamed A. |
| building | UPM Institutional Repository |
| collection | Online Access |
| description | As a hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, Fluvastatin (FLV) is used for reducing low-density lipoprotein (LDL) cholesterol as well as to prevent cardiovascular problems. FLV showed cell line cytotoxicity and antitumor effect. Melittin (MEL) exhibits antineoplastic activity and is known to be promising as a therapeutic option for cancer patients. The aim of this work was to investigate the combination of FLV with MEL loaded hybrid formula of phospholipid (PL) with alpha lipoic acid (ALA) nanoparticles to maximize anticancer tendencies. This study examines the optimization of the prepared formulation in order to minimize nanoparticles size and maximize zeta potential to potentiate cytotoxic potentialities in colon cancer cells (Caco2), cell viability, cell cycle analysis and annexin V were tested. In addition to biological markers as P53, Bax, bcl2 and Caspase 3 evaluation The combination involving FLV PL ALA MEL showed enhanced cytotoxic potentiality (IC50 = 9.242 ± 0.35 µg/mL), about twofold lower, compared to the raw FLV (IC50 = 21.74 ± 0.82 µg/mL). According to studies analyzing cell cycle, optimized FLV PL ALA MEL was found to inhibit Caco2 colon cancer cells more significantly than other therapeutic treatments, wherein a higher number of cells were found to accumulate over G2/M and pre-G1 phases, whereas G0/G1/S phases witnessed the accumulation of a lower number of cells. The optimized formulation may pave the way for a novel and more efficacious treatment for colon cancer. |
| first_indexed | 2025-11-15T13:35:52Z |
| format | Article |
| id | upm-101752 |
| institution | Universiti Putra Malaysia |
| institution_category | Local University |
| last_indexed | 2025-11-15T13:35:52Z |
| publishDate | 2022 |
| publisher | Nature Publishing Group |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | upm-1017522024-04-30T07:04:19Z http://psasir.upm.edu.my/id/eprint/101752/ Hybrid nanoparticulate system of Fluvastatin loaded phospholipid, alpha lipoic acid and melittin for the management of colon cancer Alfaleh, Mohamed A. Fahmy, Omar Abourehab, Mohammed A. S. Fahmy, Usama A. Alharbi, Awaad S. Alhakamy, Nabil A. As a hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, Fluvastatin (FLV) is used for reducing low-density lipoprotein (LDL) cholesterol as well as to prevent cardiovascular problems. FLV showed cell line cytotoxicity and antitumor effect. Melittin (MEL) exhibits antineoplastic activity and is known to be promising as a therapeutic option for cancer patients. The aim of this work was to investigate the combination of FLV with MEL loaded hybrid formula of phospholipid (PL) with alpha lipoic acid (ALA) nanoparticles to maximize anticancer tendencies. This study examines the optimization of the prepared formulation in order to minimize nanoparticles size and maximize zeta potential to potentiate cytotoxic potentialities in colon cancer cells (Caco2), cell viability, cell cycle analysis and annexin V were tested. In addition to biological markers as P53, Bax, bcl2 and Caspase 3 evaluation The combination involving FLV PL ALA MEL showed enhanced cytotoxic potentiality (IC50 = 9.242 ± 0.35 µg/mL), about twofold lower, compared to the raw FLV (IC50 = 21.74 ± 0.82 µg/mL). According to studies analyzing cell cycle, optimized FLV PL ALA MEL was found to inhibit Caco2 colon cancer cells more significantly than other therapeutic treatments, wherein a higher number of cells were found to accumulate over G2/M and pre-G1 phases, whereas G0/G1/S phases witnessed the accumulation of a lower number of cells. The optimized formulation may pave the way for a novel and more efficacious treatment for colon cancer. Nature Publishing Group 2022 Article PeerReviewed Alfaleh, Mohamed A. and Fahmy, Omar and Abourehab, Mohammed A. S. and Fahmy, Usama A. and Alharbi, Awaad S. and Alhakamy, Nabil A. (2022) Hybrid nanoparticulate system of Fluvastatin loaded phospholipid, alpha lipoic acid and melittin for the management of colon cancer. Scientific Reports, 12. art. no. 19446. pp. 1-16. ISSN 2045-2322 https://www.nature.com/articles/s41598-022-24151-3 10.1038/s41598-022-24151-3 |
| spellingShingle | Alfaleh, Mohamed A. Fahmy, Omar Abourehab, Mohammed A. S. Fahmy, Usama A. Alharbi, Awaad S. Alhakamy, Nabil A. Hybrid nanoparticulate system of Fluvastatin loaded phospholipid, alpha lipoic acid and melittin for the management of colon cancer |
| title | Hybrid nanoparticulate system of Fluvastatin loaded phospholipid, alpha lipoic acid and melittin for the management of colon cancer |
| title_full | Hybrid nanoparticulate system of Fluvastatin loaded phospholipid, alpha lipoic acid and melittin for the management of colon cancer |
| title_fullStr | Hybrid nanoparticulate system of Fluvastatin loaded phospholipid, alpha lipoic acid and melittin for the management of colon cancer |
| title_full_unstemmed | Hybrid nanoparticulate system of Fluvastatin loaded phospholipid, alpha lipoic acid and melittin for the management of colon cancer |
| title_short | Hybrid nanoparticulate system of Fluvastatin loaded phospholipid, alpha lipoic acid and melittin for the management of colon cancer |
| title_sort | hybrid nanoparticulate system of fluvastatin loaded phospholipid, alpha lipoic acid and melittin for the management of colon cancer |
| url | http://psasir.upm.edu.my/id/eprint/101752/ http://psasir.upm.edu.my/id/eprint/101752/ http://psasir.upm.edu.my/id/eprint/101752/ |