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New Formulation of a Methylseleno-Aspirin Analog with Anticancer Activity Towards Colon Cancer

Aspirin (ASA) has attracted wide interest of numerous scientists worldwide thanks to its chemopreventive and chemotherapeutic effects, particularly in colorectal cancer (CRC). Incorporation of selenium (Se) atom into ASA has greatly increased their anti-tumoral efficacy in CRC compared with the orga...

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Autores principales: Ruberte, Ana Carolina, González-Gaitano, Gustavo, Sharma, Arun K., Aydillo, Carlos, Encío, Ignacio, Sanmartín, Carmen, Plano, Daniel
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7730823/
https://www.ncbi.nlm.nih.gov/pubmed/33260948
http://dx.doi.org/10.3390/ijms21239017
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author Ruberte, Ana Carolina
González-Gaitano, Gustavo
Sharma, Arun K.
Aydillo, Carlos
Encío, Ignacio
Sanmartín, Carmen
Plano, Daniel
author_facet Ruberte, Ana Carolina
González-Gaitano, Gustavo
Sharma, Arun K.
Aydillo, Carlos
Encío, Ignacio
Sanmartín, Carmen
Plano, Daniel
author_sort Ruberte, Ana Carolina
collection PubMed
description Aspirin (ASA) has attracted wide interest of numerous scientists worldwide thanks to its chemopreventive and chemotherapeutic effects, particularly in colorectal cancer (CRC). Incorporation of selenium (Se) atom into ASA has greatly increased their anti-tumoral efficacy in CRC compared with the organic counterparts without the Se functionality, such as the promising antitumoral methylseleno-ASA analog (1a). Nevertheless, the efficacy of compound 1a in cancer cells is compromised due to its poor solubility and volatile nature. Thus, 1a has been formulated with native α-, β- and γ-cyclodextrin (CD), a modified β-CD (hydroxypropyl β-CD, HP-β-CD) and Pluronic F127, all of them non-toxic, biodegradable and FDA approved. Water solubility of 1a is enhanced with β- and HP- β-CDs and Pluronic F127. Compound 1a forms inclusion complexes with the CDs and was incorporated in the hydrophobic core of the F127 micelles. Herein, we evaluated the cytotoxic potential of 1a, alone or formulated with β- and HP- β-CDs or Pluronic F127, against CRC cells. Remarkably, 1a formulations demonstrated more sustained antitumoral activity toward CRC cells. Hence, β-CD, HP-β-CD and Pluronic F127 might be excellent vehicles to improve pharmacological properties of organoselenium compounds with solubility issues and volatile nature.
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spelling pubmed-77308232020-12-12 New Formulation of a Methylseleno-Aspirin Analog with Anticancer Activity Towards Colon Cancer Ruberte, Ana Carolina González-Gaitano, Gustavo Sharma, Arun K. Aydillo, Carlos Encío, Ignacio Sanmartín, Carmen Plano, Daniel Int J Mol Sci Article Aspirin (ASA) has attracted wide interest of numerous scientists worldwide thanks to its chemopreventive and chemotherapeutic effects, particularly in colorectal cancer (CRC). Incorporation of selenium (Se) atom into ASA has greatly increased their anti-tumoral efficacy in CRC compared with the organic counterparts without the Se functionality, such as the promising antitumoral methylseleno-ASA analog (1a). Nevertheless, the efficacy of compound 1a in cancer cells is compromised due to its poor solubility and volatile nature. Thus, 1a has been formulated with native α-, β- and γ-cyclodextrin (CD), a modified β-CD (hydroxypropyl β-CD, HP-β-CD) and Pluronic F127, all of them non-toxic, biodegradable and FDA approved. Water solubility of 1a is enhanced with β- and HP- β-CDs and Pluronic F127. Compound 1a forms inclusion complexes with the CDs and was incorporated in the hydrophobic core of the F127 micelles. Herein, we evaluated the cytotoxic potential of 1a, alone or formulated with β- and HP- β-CDs or Pluronic F127, against CRC cells. Remarkably, 1a formulations demonstrated more sustained antitumoral activity toward CRC cells. Hence, β-CD, HP-β-CD and Pluronic F127 might be excellent vehicles to improve pharmacological properties of organoselenium compounds with solubility issues and volatile nature. MDPI 2020-11-27 /pmc/articles/PMC7730823/ /pubmed/33260948 http://dx.doi.org/10.3390/ijms21239017 Text en © 2020 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Ruberte, Ana Carolina
González-Gaitano, Gustavo
Sharma, Arun K.
Aydillo, Carlos
Encío, Ignacio
Sanmartín, Carmen
Plano, Daniel
New Formulation of a Methylseleno-Aspirin Analog with Anticancer Activity Towards Colon Cancer
title New Formulation of a Methylseleno-Aspirin Analog with Anticancer Activity Towards Colon Cancer
title_full New Formulation of a Methylseleno-Aspirin Analog with Anticancer Activity Towards Colon Cancer
title_fullStr New Formulation of a Methylseleno-Aspirin Analog with Anticancer Activity Towards Colon Cancer
title_full_unstemmed New Formulation of a Methylseleno-Aspirin Analog with Anticancer Activity Towards Colon Cancer
title_short New Formulation of a Methylseleno-Aspirin Analog with Anticancer Activity Towards Colon Cancer
title_sort new formulation of a methylseleno-aspirin analog with anticancer activity towards colon cancer
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7730823/
https://www.ncbi.nlm.nih.gov/pubmed/33260948
http://dx.doi.org/10.3390/ijms21239017
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