Selective Targeting of Breast Cancer by Tafuramycin A Using SMA-Nanoassemblies
Triple-negative breast cancer (TNBC) is a heterogeneous subtype of tumors that tests negative for estrogen receptors, progesterone receptors, and excess HER2 protein. The mainstay of treatment remains chemotherapy, but the therapeutic outcome remains inadequate. This paper investigates the potential...
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MDPI AG
2021-06-01
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Series: | Molecules |
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Online Access: | https://www.mdpi.com/1420-3049/26/12/3532 |
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author | Ibrahim M. El-Deeb Valeria Pittala Diab Eltayeb Khaled Greish |
author_facet | Ibrahim M. El-Deeb Valeria Pittala Diab Eltayeb Khaled Greish |
author_sort | Ibrahim M. El-Deeb |
collection | DOAJ |
description | Triple-negative breast cancer (TNBC) is a heterogeneous subtype of tumors that tests negative for estrogen receptors, progesterone receptors, and excess HER2 protein. The mainstay of treatment remains chemotherapy, but the therapeutic outcome remains inadequate. This paper investigates the potential of a duocarmycin derivative, tafuramycin A (TFA), as a new and more effective chemotherapy agent in TNBC treatment. To this extent, we optimized the chemical synthesis of TFA, and we encapsulated TFA in a micellar system to reduce side effects and increase tumor accumulation. In vitro and in vivo studies suggest that both TFA and SMA–TFA possess high anticancer effects in TNBC models. Finally, the encapsulation of TFA offered a preferential avenue to tumor accumulation by increasing its concentration at the tumor tissues by around four times in comparison with the free drug. Overall, the results provide a new potential strategy useful for TNBC treatment. |
first_indexed | 2024-03-10T10:33:09Z |
format | Article |
id | doaj.art-55d21d092a0c4020aeecebafe7bdf517 |
institution | Directory Open Access Journal |
issn | 1420-3049 |
language | English |
last_indexed | 2024-03-10T10:33:09Z |
publishDate | 2021-06-01 |
publisher | MDPI AG |
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series | Molecules |
spelling | doaj.art-55d21d092a0c4020aeecebafe7bdf5172023-11-21T23:27:30ZengMDPI AGMolecules1420-30492021-06-012612353210.3390/molecules26123532Selective Targeting of Breast Cancer by Tafuramycin A Using SMA-NanoassembliesIbrahim M. El-Deeb0Valeria Pittala1Diab Eltayeb2Khaled Greish3Department of Medical Sciences, Royal College of Surgeons in Ireland, Medical University of Bahrain, Busaiteen 228, BahrainDepartment of Drug and Health Science, University of Catania, 95125 Catania, ItalyDepartment of Molecular Medicine, Arabian Gulf University, Manama 329, BahrainDepartment of Molecular Medicine, Arabian Gulf University, Manama 329, BahrainTriple-negative breast cancer (TNBC) is a heterogeneous subtype of tumors that tests negative for estrogen receptors, progesterone receptors, and excess HER2 protein. The mainstay of treatment remains chemotherapy, but the therapeutic outcome remains inadequate. This paper investigates the potential of a duocarmycin derivative, tafuramycin A (TFA), as a new and more effective chemotherapy agent in TNBC treatment. To this extent, we optimized the chemical synthesis of TFA, and we encapsulated TFA in a micellar system to reduce side effects and increase tumor accumulation. In vitro and in vivo studies suggest that both TFA and SMA–TFA possess high anticancer effects in TNBC models. Finally, the encapsulation of TFA offered a preferential avenue to tumor accumulation by increasing its concentration at the tumor tissues by around four times in comparison with the free drug. Overall, the results provide a new potential strategy useful for TNBC treatment.https://www.mdpi.com/1420-3049/26/12/3532duocarmycintafuramycin ATNBCpoly(styrene-co-maleic acid) micellesnanoformulationEPR effect |
spellingShingle | Ibrahim M. El-Deeb Valeria Pittala Diab Eltayeb Khaled Greish Selective Targeting of Breast Cancer by Tafuramycin A Using SMA-Nanoassemblies Molecules duocarmycin tafuramycin A TNBC poly(styrene-co-maleic acid) micelles nanoformulation EPR effect |
title | Selective Targeting of Breast Cancer by Tafuramycin A Using SMA-Nanoassemblies |
title_full | Selective Targeting of Breast Cancer by Tafuramycin A Using SMA-Nanoassemblies |
title_fullStr | Selective Targeting of Breast Cancer by Tafuramycin A Using SMA-Nanoassemblies |
title_full_unstemmed | Selective Targeting of Breast Cancer by Tafuramycin A Using SMA-Nanoassemblies |
title_short | Selective Targeting of Breast Cancer by Tafuramycin A Using SMA-Nanoassemblies |
title_sort | selective targeting of breast cancer by tafuramycin a using sma nanoassemblies |
topic | duocarmycin tafuramycin A TNBC poly(styrene-co-maleic acid) micelles nanoformulation EPR effect |
url | https://www.mdpi.com/1420-3049/26/12/3532 |
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