Formulation, characterization, and cellular toxicity assessment of tamoxifen-loaded silk fibroin nanoparticles in breast cancer

Silk fibroin (SF) is a natural polymeric biomaterial that is widely adopted for the preparation of drug delivery systems. Herein, we aimed to fabricate and characterize SF nanoparticles loaded with the selective estrogen receptor modulator; tamoxifen citrate (TC-SF-NPs) and to assess their in vitro...

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Main Authors: Afrasim Moin, Shahid Ud Din Wani, Riyaz Ali Osmani, Amr S. Abu Lila, El-Sayed Khafagy, Hany H. Arab, Hosahalli V. Gangadharappa, Ahmed N. Allam
Format: Article
Language:English
Published: Taylor & Francis Group 2021-01-01
Series:Drug Delivery
Subjects:
Online Access:http://dx.doi.org/10.1080/10717544.2021.1958106
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author Afrasim Moin
Shahid Ud Din Wani
Riyaz Ali Osmani
Amr S. Abu Lila
El-Sayed Khafagy
Hany H. Arab
Hosahalli V. Gangadharappa
Ahmed N. Allam
author_facet Afrasim Moin
Shahid Ud Din Wani
Riyaz Ali Osmani
Amr S. Abu Lila
El-Sayed Khafagy
Hany H. Arab
Hosahalli V. Gangadharappa
Ahmed N. Allam
author_sort Afrasim Moin
collection DOAJ
description Silk fibroin (SF) is a natural polymeric biomaterial that is widely adopted for the preparation of drug delivery systems. Herein, we aimed to fabricate and characterize SF nanoparticles loaded with the selective estrogen receptor modulator; tamoxifen citrate (TC-SF-NPs) and to assess their in vitro efficacy against breast cancer cell lines (MCF-7 and MDA-MB-231). TC-loaded SF-NPs were characterized for particle size, morphology, entrapment efficiency, and release profile. In addition, we examined the in vitro cytotoxicity of TC-SF-NPs against human breast cancer cell lines and evaluated the anticancer potential of TC-SF-NPs through apoptosis assay and cell cycle analysis. Drug-loaded SF-NPs showed an average particle size of 186.1 ± 5.9 nm and entrapment efficiency of 79.08%. Scanning electron microscopy (SEM) showed the nanoparticles had a spherical morphology with smooth surface. Tamoxifen release from SF-NPs exhibited a biphasic release profile with an initial burst release within the first 6 h and sustained release for 48 h. TC-SF-NPs exerted a dose-dependent cytotoxic effect against breast cancer cell lines. In addition, flow cytometry analysis revealed that cells accumulate in G0/G1 phase, with a concomitant reduction of S- and G2-M-phase cells upon treatment with TC-SF-NPs. Consequently, the potent anticancer activities of TC-SF-NPs against breast cancer cells were mainly attributed to the induction of apoptosis and cell cycle arrest. Our results indicate that SF nanoparticles may represent an attractive nontoxic nanocarrier for the delivery of anticancer drugs.
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spelling doaj.art-58cc74e71f114a0dbd286747bc2d00572022-12-21T23:44:37ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642021-01-012811626163610.1080/10717544.2021.19581061958106Formulation, characterization, and cellular toxicity assessment of tamoxifen-loaded silk fibroin nanoparticles in breast cancerAfrasim Moin0Shahid Ud Din Wani1Riyaz Ali Osmani2Amr S. Abu Lila3El-Sayed Khafagy4Hany H. Arab5Hosahalli V. Gangadharappa6Ahmed N. Allam7Department of Pharmaceutics, College of Pharmacy, University of HailDepartment of Pharmaceutics, CT Institute of Pharmaceutical SciencesDepartment of Biosciences and Bioengineering, Indian Institute of Technology BombayDepartment of Pharmaceutics, College of Pharmacy, University of HailDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz UniversityDepartment of Pharmacology and Toxicology, College of Pharmacy, Taif UniversityDepartment of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education and ResearchDepartment of Pharmaceutics, Faculty of Pharmacy, Alexandria UniversitySilk fibroin (SF) is a natural polymeric biomaterial that is widely adopted for the preparation of drug delivery systems. Herein, we aimed to fabricate and characterize SF nanoparticles loaded with the selective estrogen receptor modulator; tamoxifen citrate (TC-SF-NPs) and to assess their in vitro efficacy against breast cancer cell lines (MCF-7 and MDA-MB-231). TC-loaded SF-NPs were characterized for particle size, morphology, entrapment efficiency, and release profile. In addition, we examined the in vitro cytotoxicity of TC-SF-NPs against human breast cancer cell lines and evaluated the anticancer potential of TC-SF-NPs through apoptosis assay and cell cycle analysis. Drug-loaded SF-NPs showed an average particle size of 186.1 ± 5.9 nm and entrapment efficiency of 79.08%. Scanning electron microscopy (SEM) showed the nanoparticles had a spherical morphology with smooth surface. Tamoxifen release from SF-NPs exhibited a biphasic release profile with an initial burst release within the first 6 h and sustained release for 48 h. TC-SF-NPs exerted a dose-dependent cytotoxic effect against breast cancer cell lines. In addition, flow cytometry analysis revealed that cells accumulate in G0/G1 phase, with a concomitant reduction of S- and G2-M-phase cells upon treatment with TC-SF-NPs. Consequently, the potent anticancer activities of TC-SF-NPs against breast cancer cells were mainly attributed to the induction of apoptosis and cell cycle arrest. Our results indicate that SF nanoparticles may represent an attractive nontoxic nanocarrier for the delivery of anticancer drugs.http://dx.doi.org/10.1080/10717544.2021.1958106breast cancerin vitro cytotoxicitynanoparticlessilk fibrointamoxifen citrate
spellingShingle Afrasim Moin
Shahid Ud Din Wani
Riyaz Ali Osmani
Amr S. Abu Lila
El-Sayed Khafagy
Hany H. Arab
Hosahalli V. Gangadharappa
Ahmed N. Allam
Formulation, characterization, and cellular toxicity assessment of tamoxifen-loaded silk fibroin nanoparticles in breast cancer
Drug Delivery
breast cancer
in vitro cytotoxicity
nanoparticles
silk fibroin
tamoxifen citrate
title Formulation, characterization, and cellular toxicity assessment of tamoxifen-loaded silk fibroin nanoparticles in breast cancer
title_full Formulation, characterization, and cellular toxicity assessment of tamoxifen-loaded silk fibroin nanoparticles in breast cancer
title_fullStr Formulation, characterization, and cellular toxicity assessment of tamoxifen-loaded silk fibroin nanoparticles in breast cancer
title_full_unstemmed Formulation, characterization, and cellular toxicity assessment of tamoxifen-loaded silk fibroin nanoparticles in breast cancer
title_short Formulation, characterization, and cellular toxicity assessment of tamoxifen-loaded silk fibroin nanoparticles in breast cancer
title_sort formulation characterization and cellular toxicity assessment of tamoxifen loaded silk fibroin nanoparticles in breast cancer
topic breast cancer
in vitro cytotoxicity
nanoparticles
silk fibroin
tamoxifen citrate
url http://dx.doi.org/10.1080/10717544.2021.1958106
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