Fmoc-FF Nanogel-Mediated Delivery of Doxorubicin and Curcumin in Thyroid Cancer Cells

<b>Background:</b> Thyroid cancer (TC) is the most prevalent endocrine malignancy, and is categorized into well-differentiated and aggressive anaplastic types. Novel therapeutic modalities are needed for TC. Nanomedicine is a promising strategy for the development of precision medicine....

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Main Authors: Enrico Gallo, Giovanni Smaldone, Luca Cimmino, Mariantonia Braile, Francesca Maria Orlandella, Neila Luciano, Antonella Accardo, Giuliana Salvatore
Format: Article
Language:English
Published: MDPI AG 2025-02-01
Series:Pharmaceutics
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Online Access:https://www.mdpi.com/1999-4923/17/2/263
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author Enrico Gallo
Giovanni Smaldone
Luca Cimmino
Mariantonia Braile
Francesca Maria Orlandella
Neila Luciano
Antonella Accardo
Giuliana Salvatore
author_facet Enrico Gallo
Giovanni Smaldone
Luca Cimmino
Mariantonia Braile
Francesca Maria Orlandella
Neila Luciano
Antonella Accardo
Giuliana Salvatore
author_sort Enrico Gallo
collection DOAJ
description <b>Background:</b> Thyroid cancer (TC) is the most prevalent endocrine malignancy, and is categorized into well-differentiated and aggressive anaplastic types. Novel therapeutic modalities are needed for TC. Nanomedicine is a promising strategy for the development of precision medicine. In this context, we investigated the use of nanogels (NGs) to deliver agents with different physicochemical properties, specifically the hydrophilic agent doxorubicin (DOX) and the hydrophobic compound curcumin (CUR), in TC cell lines. <b>Methods:</b> Nα-9-fluorenylmethoxycarbonyl-diphenylalanine (Fmoc-FF) peptide-based NGs loaded with DOX and CUR were formulated using the solvent-switch method. DOX-loaded NGs were previously characterized. CUR-loaded NGs were characterized through rheology, scanning electron microscopy (SEM), dynamic light scattering (DLS), nanoparticle tracking analysis (NTA), and Fourier transform infrared (FT-IR) spectroscopy. Confocal microscopy, q-RT-PCR, and ATP lite assays were performed to evaluate the uptake and delivery of DOX- and CUR-loaded NGs on TC cell lines. <b>Results:</b> CUR-loaded NGs exhibited a mean diameter of approximately 204.3 nm and a zeta potential of −34.6 mV, indicative of a good stability. In vitro release studies revealed a sustained release profile of CUR over 72 h. Functional analyses demonstrated that Fmoc-FF-loaded NGs were internalized into TC cell lines. They were primarily localized in the cytoplasm rather than in early endosomes, thereby ensuring intracellular stability. Furthermore, Fmoc-FF NGs reduced the nuclear uptake kinetics of DOX in TC cells, suggesting a potential reduction in dose-limiting toxicity. Comparative studies with CUR-loaded NGs revealed similar internalization and delayed nuclear uptake, highlighting the efficacy of Fmoc-FF NGs in delivering hydrophobic agents. <b>Conclusions:</b> Overall, the data suggest that Fmoc-FF NGs represent a promising strategy for delivering agents with diverse physicochemical properties in TC, enhancing their efficacy and safety and warranting further investigation.
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spelling doaj-art-d83cf2ed30cc40f49b5a9797452f75822025-08-20T03:12:19ZengMDPI AGPharmaceutics1999-49232025-02-0117226310.3390/pharmaceutics17020263Fmoc-FF Nanogel-Mediated Delivery of Doxorubicin and Curcumin in Thyroid Cancer CellsEnrico Gallo0Giovanni Smaldone1Luca Cimmino2Mariantonia Braile3Francesca Maria Orlandella4Neila Luciano5Antonella Accardo6Giuliana Salvatore7IRCCS SYNLAB SDN, 80146 Naples, ItalyIRCCS SYNLAB SDN, 80146 Naples, ItalyIRCCS SYNLAB SDN, 80146 Naples, ItalyIRCCS SYNLAB SDN, 80146 Naples, ItalyDipartimento delle Scienze Mediche, Motorie e del Benessere, Università degli Studi di Napoli “Parthenope”, 80133 Naples, ItalyDipartimento di Scienze Biomediche Avanzate, Università degli Studi di Napoli “Federico II”, 80131 Naples, ItalyDipartimento di Farmacia, Università degli Studi di Napoli “Federico II”, 80131 Naples, ItalyDipartimento delle Scienze Mediche, Motorie e del Benessere, Università degli Studi di Napoli “Parthenope”, 80133 Naples, Italy<b>Background:</b> Thyroid cancer (TC) is the most prevalent endocrine malignancy, and is categorized into well-differentiated and aggressive anaplastic types. Novel therapeutic modalities are needed for TC. Nanomedicine is a promising strategy for the development of precision medicine. In this context, we investigated the use of nanogels (NGs) to deliver agents with different physicochemical properties, specifically the hydrophilic agent doxorubicin (DOX) and the hydrophobic compound curcumin (CUR), in TC cell lines. <b>Methods:</b> Nα-9-fluorenylmethoxycarbonyl-diphenylalanine (Fmoc-FF) peptide-based NGs loaded with DOX and CUR were formulated using the solvent-switch method. DOX-loaded NGs were previously characterized. CUR-loaded NGs were characterized through rheology, scanning electron microscopy (SEM), dynamic light scattering (DLS), nanoparticle tracking analysis (NTA), and Fourier transform infrared (FT-IR) spectroscopy. Confocal microscopy, q-RT-PCR, and ATP lite assays were performed to evaluate the uptake and delivery of DOX- and CUR-loaded NGs on TC cell lines. <b>Results:</b> CUR-loaded NGs exhibited a mean diameter of approximately 204.3 nm and a zeta potential of −34.6 mV, indicative of a good stability. In vitro release studies revealed a sustained release profile of CUR over 72 h. Functional analyses demonstrated that Fmoc-FF-loaded NGs were internalized into TC cell lines. They were primarily localized in the cytoplasm rather than in early endosomes, thereby ensuring intracellular stability. Furthermore, Fmoc-FF NGs reduced the nuclear uptake kinetics of DOX in TC cells, suggesting a potential reduction in dose-limiting toxicity. Comparative studies with CUR-loaded NGs revealed similar internalization and delayed nuclear uptake, highlighting the efficacy of Fmoc-FF NGs in delivering hydrophobic agents. <b>Conclusions:</b> Overall, the data suggest that Fmoc-FF NGs represent a promising strategy for delivering agents with diverse physicochemical properties in TC, enhancing their efficacy and safety and warranting further investigation.https://www.mdpi.com/1999-4923/17/2/263thyroid cancernanogeldoxorubicincurcuminnanodelivery
spellingShingle Enrico Gallo
Giovanni Smaldone
Luca Cimmino
Mariantonia Braile
Francesca Maria Orlandella
Neila Luciano
Antonella Accardo
Giuliana Salvatore
Fmoc-FF Nanogel-Mediated Delivery of Doxorubicin and Curcumin in Thyroid Cancer Cells
Pharmaceutics
thyroid cancer
nanogel
doxorubicin
curcumin
nanodelivery
title Fmoc-FF Nanogel-Mediated Delivery of Doxorubicin and Curcumin in Thyroid Cancer Cells
title_full Fmoc-FF Nanogel-Mediated Delivery of Doxorubicin and Curcumin in Thyroid Cancer Cells
title_fullStr Fmoc-FF Nanogel-Mediated Delivery of Doxorubicin and Curcumin in Thyroid Cancer Cells
title_full_unstemmed Fmoc-FF Nanogel-Mediated Delivery of Doxorubicin and Curcumin in Thyroid Cancer Cells
title_short Fmoc-FF Nanogel-Mediated Delivery of Doxorubicin and Curcumin in Thyroid Cancer Cells
title_sort fmoc ff nanogel mediated delivery of doxorubicin and curcumin in thyroid cancer cells
topic thyroid cancer
nanogel
doxorubicin
curcumin
nanodelivery
url https://www.mdpi.com/1999-4923/17/2/263
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