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Norcantharidin Nanoemulsion Development, Characterization, and In Vitro Antiproliferation Effect on B16F1 Melanoma Cells

Melanoma is a highly lethal type of cancer that has had an increase in incidence in the last decades. Nevertheless, current therapies lack effectiveness and have highly disabling side effects, which calls for new therapeutic strategies. Norcantharidin (NCTD) is an acid derivative with potential anti...

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Autores principales: Martínez-Razo, Gabriel, Pires, Patrícia C., Domínguez-López, María Lilia, Veiga, Francisco, Vega-López, Armando, Paiva-Santos, Ana Cláudia
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10143330/
https://www.ncbi.nlm.nih.gov/pubmed/37111258
http://dx.doi.org/10.3390/ph16040501
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author Martínez-Razo, Gabriel
Pires, Patrícia C.
Domínguez-López, María Lilia
Veiga, Francisco
Vega-López, Armando
Paiva-Santos, Ana Cláudia
author_facet Martínez-Razo, Gabriel
Pires, Patrícia C.
Domínguez-López, María Lilia
Veiga, Francisco
Vega-López, Armando
Paiva-Santos, Ana Cláudia
author_sort Martínez-Razo, Gabriel
collection PubMed
description Melanoma is a highly lethal type of cancer that has had an increase in incidence in the last decades. Nevertheless, current therapies lack effectiveness and have highly disabling side effects, which calls for new therapeutic strategies. Norcantharidin (NCTD) is an acid derivative with potential antitumor activity isolated from natural blister beetles. However, its solubility limitations restrict its use. To address this issue, we developed an oil-in-water nanoemulsion using commonly available cosmetic ingredients, which increased NCTD solubility 10-fold compared to water. The developed nanoemulsion showed a good droplet size and homogeneity, with adequate pH and viscosity for skin application. In vitro drug release studies showed a sustained release profile, ideal for prolonged therapeutic effects. Accelerated stability studies proved that the formulation was reasonably stable under stress conditions, with particle separation fingerprints, instability index, particle size, and sedimentation velocity analyses being conducted. To assess the therapeutic potential of the developed formulation, in vitro studies were conducted on melanoma B16F1 cells; results showed an IC50 of 1.026 +/− 0.370 mg/kg, and the cells’ metabolic activity decreased after exposure to the NCTD nanoemulsion. Hence, a new “easy-to-make” nanoformulation with therapeutic potential on melanoma cells was developed, as a possible adjuvant for future melanoma treatment.
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spelling pubmed-101433302023-04-29 Norcantharidin Nanoemulsion Development, Characterization, and In Vitro Antiproliferation Effect on B16F1 Melanoma Cells Martínez-Razo, Gabriel Pires, Patrícia C. Domínguez-López, María Lilia Veiga, Francisco Vega-López, Armando Paiva-Santos, Ana Cláudia Pharmaceuticals (Basel) Article Melanoma is a highly lethal type of cancer that has had an increase in incidence in the last decades. Nevertheless, current therapies lack effectiveness and have highly disabling side effects, which calls for new therapeutic strategies. Norcantharidin (NCTD) is an acid derivative with potential antitumor activity isolated from natural blister beetles. However, its solubility limitations restrict its use. To address this issue, we developed an oil-in-water nanoemulsion using commonly available cosmetic ingredients, which increased NCTD solubility 10-fold compared to water. The developed nanoemulsion showed a good droplet size and homogeneity, with adequate pH and viscosity for skin application. In vitro drug release studies showed a sustained release profile, ideal for prolonged therapeutic effects. Accelerated stability studies proved that the formulation was reasonably stable under stress conditions, with particle separation fingerprints, instability index, particle size, and sedimentation velocity analyses being conducted. To assess the therapeutic potential of the developed formulation, in vitro studies were conducted on melanoma B16F1 cells; results showed an IC50 of 1.026 +/− 0.370 mg/kg, and the cells’ metabolic activity decreased after exposure to the NCTD nanoemulsion. Hence, a new “easy-to-make” nanoformulation with therapeutic potential on melanoma cells was developed, as a possible adjuvant for future melanoma treatment. MDPI 2023-03-28 /pmc/articles/PMC10143330/ /pubmed/37111258 http://dx.doi.org/10.3390/ph16040501 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
Martínez-Razo, Gabriel
Pires, Patrícia C.
Domínguez-López, María Lilia
Veiga, Francisco
Vega-López, Armando
Paiva-Santos, Ana Cláudia
Norcantharidin Nanoemulsion Development, Characterization, and In Vitro Antiproliferation Effect on B16F1 Melanoma Cells
title Norcantharidin Nanoemulsion Development, Characterization, and In Vitro Antiproliferation Effect on B16F1 Melanoma Cells
title_full Norcantharidin Nanoemulsion Development, Characterization, and In Vitro Antiproliferation Effect on B16F1 Melanoma Cells
title_fullStr Norcantharidin Nanoemulsion Development, Characterization, and In Vitro Antiproliferation Effect on B16F1 Melanoma Cells
title_full_unstemmed Norcantharidin Nanoemulsion Development, Characterization, and In Vitro Antiproliferation Effect on B16F1 Melanoma Cells
title_short Norcantharidin Nanoemulsion Development, Characterization, and In Vitro Antiproliferation Effect on B16F1 Melanoma Cells
title_sort norcantharidin nanoemulsion development, characterization, and in vitro antiproliferation effect on b16f1 melanoma cells
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10143330/
https://www.ncbi.nlm.nih.gov/pubmed/37111258
http://dx.doi.org/10.3390/ph16040501
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