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Targeted Fisetin-Encapsulated β-Cyclodextrin Nanosponges for Breast Cancer
Fisetin (FS) is considered a safer phytomedicine alternative to conventional chemotherapeutics for breast cancer treatment. Despite its surpassing therapeutic potential, its clinical utility is hampered by its low systemic bioavailability. Accordingly, as far as we are aware, this is the first study...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10223291/ https://www.ncbi.nlm.nih.gov/pubmed/37242722 http://dx.doi.org/10.3390/pharmaceutics15051480 |
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author | Aboushanab, Alaa R. El-Moslemany, Riham M. El-Kamel, Amal H. Mehanna, Radwa A. Bakr, Basant A. Ashour, Asmaa A. |
author_facet | Aboushanab, Alaa R. El-Moslemany, Riham M. El-Kamel, Amal H. Mehanna, Radwa A. Bakr, Basant A. Ashour, Asmaa A. |
author_sort | Aboushanab, Alaa R. |
collection | PubMed |
description | Fisetin (FS) is considered a safer phytomedicine alternative to conventional chemotherapeutics for breast cancer treatment. Despite its surpassing therapeutic potential, its clinical utility is hampered by its low systemic bioavailability. Accordingly, as far as we are aware, this is the first study to develop lactoferrin-coated FS-loaded β-cyclodextrin nanosponges (LF-FS-NS) for targeted FS delivery to breast cancer. NS formation through cross-linking of β-cyclodextrin by diphenyl carbonate was confirmed by FTIR and XRD. The selected LF-FS-NS showed good colloidal properties (size 52.7 ± 7.2 nm, PDI < 0.3, and ζ-potential 24 mV), high loading efficiency (96 ± 0.3%), and sustained drug release of 26 % after 24 h. Morphological examination using SEM revealed the mesoporous spherical structure of the prepared nanosponges with a pore diameter of ~30 nm, which was further confirmed by surface area measurement. Additionally, LF-FS-NS enhanced FS oral and IP bioavailability (2.5- and 3.2-fold, respectively) compared to FS suspension in rats. Antitumor efficacy evaluation in vitro on MDA-MB-231 cells and in vivo on an Ehrlich ascites mouse model demonstrated significantly higher activity and targetability of LF-FS-NS (30 mg/kg) compared to the free drug and uncoated formulation. Consequently, LF-FS-NS could be addressed as a promising formulation for the effective management of breast cancer. |
format | Online Article Text |
id | pubmed-10223291 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-102232912023-05-28 Targeted Fisetin-Encapsulated β-Cyclodextrin Nanosponges for Breast Cancer Aboushanab, Alaa R. El-Moslemany, Riham M. El-Kamel, Amal H. Mehanna, Radwa A. Bakr, Basant A. Ashour, Asmaa A. Pharmaceutics Article Fisetin (FS) is considered a safer phytomedicine alternative to conventional chemotherapeutics for breast cancer treatment. Despite its surpassing therapeutic potential, its clinical utility is hampered by its low systemic bioavailability. Accordingly, as far as we are aware, this is the first study to develop lactoferrin-coated FS-loaded β-cyclodextrin nanosponges (LF-FS-NS) for targeted FS delivery to breast cancer. NS formation through cross-linking of β-cyclodextrin by diphenyl carbonate was confirmed by FTIR and XRD. The selected LF-FS-NS showed good colloidal properties (size 52.7 ± 7.2 nm, PDI < 0.3, and ζ-potential 24 mV), high loading efficiency (96 ± 0.3%), and sustained drug release of 26 % after 24 h. Morphological examination using SEM revealed the mesoporous spherical structure of the prepared nanosponges with a pore diameter of ~30 nm, which was further confirmed by surface area measurement. Additionally, LF-FS-NS enhanced FS oral and IP bioavailability (2.5- and 3.2-fold, respectively) compared to FS suspension in rats. Antitumor efficacy evaluation in vitro on MDA-MB-231 cells and in vivo on an Ehrlich ascites mouse model demonstrated significantly higher activity and targetability of LF-FS-NS (30 mg/kg) compared to the free drug and uncoated formulation. Consequently, LF-FS-NS could be addressed as a promising formulation for the effective management of breast cancer. MDPI 2023-05-12 /pmc/articles/PMC10223291/ /pubmed/37242722 http://dx.doi.org/10.3390/pharmaceutics15051480 Text en © 2023 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 Aboushanab, Alaa R. El-Moslemany, Riham M. El-Kamel, Amal H. Mehanna, Radwa A. Bakr, Basant A. Ashour, Asmaa A. Targeted Fisetin-Encapsulated β-Cyclodextrin Nanosponges for Breast Cancer |
title | Targeted Fisetin-Encapsulated β-Cyclodextrin Nanosponges for Breast Cancer |
title_full | Targeted Fisetin-Encapsulated β-Cyclodextrin Nanosponges for Breast Cancer |
title_fullStr | Targeted Fisetin-Encapsulated β-Cyclodextrin Nanosponges for Breast Cancer |
title_full_unstemmed | Targeted Fisetin-Encapsulated β-Cyclodextrin Nanosponges for Breast Cancer |
title_short | Targeted Fisetin-Encapsulated β-Cyclodextrin Nanosponges for Breast Cancer |
title_sort | targeted fisetin-encapsulated β-cyclodextrin nanosponges for breast cancer |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10223291/ https://www.ncbi.nlm.nih.gov/pubmed/37242722 http://dx.doi.org/10.3390/pharmaceutics15051480 |
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