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 Martínez, Ignacio; Sanmartín, Carmen; Plano, Daniel

New formulation of a methylseleno-aspirin analog with anticancer activity towards colon cancer

dc.contributor.author	Ruberte, Ana Carolina
dc.contributor.author	González Gaitano, Gustavo
dc.contributor.author	Sharma, Arun K.
dc.contributor.author	Aydillo, Carlos
dc.contributor.author	Encío Martínez, Ignacio
dc.contributor.author	Sanmartín, Carmen
dc.contributor.author	Plano, Daniel
dc.contributor.department	Ciencias de la Salud	es_ES
dc.contributor.department	Osasun Zientziak	eu
dc.date.accessioned	2021-06-14T11:17:34Z
dc.date.available	2021-06-14T11:17:34Z
dc.date.issued	2020
dc.description	Incluye material complementario	es_ES
dc.description.abstract	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.	en
dc.description.sponsorship	C.S. and D.P. wish to express their gratitude to PIUNA (2018-19) and UNED-Pamplona, Fundación Bancaria La Caixa, and Fundación Caja Navarra for financial support for the project.	en
dc.format.extent	17 p.
dc.format.mimetype	application/pdf	en
dc.identifier.doi	10.3390/ijms21239017
dc.identifier.issn	0
dc.identifier.uri	https://academica-e.unavarra.es/handle/2454/39906
dc.language.iso	eng	en
dc.publisher	MDPI	en
dc.relation.ispartof	International Journal of Molecular Sciences, 2020, 21, 9017	en
dc.relation.publisherversion	https://doi.org/10.3390/ijms21239017
dc.rights	© 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.	en
dc.rights.accessRights	info:eu-repo/semantics/openAccess
dc.rights.uri	https://creativecommons.org/licenses/by/4.0/
dc.subject	Aspirin	en
dc.subject	Colorectal cancer	en
dc.subject	Cyclodextrins	en
dc.subject	Cytotoxicity	en
dc.subject	Pluronic	en
dc.subject	Selenium	en
dc.title	New formulation of a methylseleno-aspirin analog with anticancer activity towards colon cancer	en
dc.type	info:eu-repo/semantics/article
dc.type.version	info:eu-repo/semantics/publishedVersion
dspace.entity.type	Publication
relation.isAuthorOfPublication	599ca381-1fd2-4a23-93ab-4373837eb6e0
relation.isAuthorOfPublication.latestForDiscovery	599ca381-1fd2-4a23-93ab-4373837eb6e0