Author, as appears in the article.: Pérez-Sánchez A; Cuyàs E; Ruiz-Torres V; Agulló-Chazarra L; Verdura S; González-álvarez I; Bermejo M; Joven J; Micol V; Bosch-Barrera J; Menendez J

Department: Medicina i Cirurgia

URV's Author/s: Joven Maried, Jorge

Keywords: Silibinin Cancer Blood–brain barrier Blood-brain barrier Bioavailability

Abstract: An ever-growing number of preclinical studies have investigated the tumoricidal activity of the milk thistle flavonolignan silibinin. The clinical value of silibinin as a bona fide anti-cancer therapy, however, remains uncertain with respect to its bioavailability and blood⁻brain barrier (BBB) permeability. To shed some light on the absorption and bioavailability of silibinin, we utilized the Caco-2 cell monolayer model of human intestinal absorption to evaluate the permeation properties of three different formulations of silibinin: silibinin-meglumine, a water-soluble form of silibinin complexed with the amino-sugar meglumine; silibinin-phosphatidylcholine, the phytolipid delivery system Siliphos; and Eurosil85/Euromed, a milk thistle extract that is the active component of the nutraceutical Legasil with enhanced bioavailability. Our approach predicted differential mechanisms of transport and blood⁻brain barrier permeabilities between the silibinin formulations tested. Our assessment might provide valuable information about an idoneous silibinin formulation capable of reaching target cancer tissues and accounting for the observed clinical effects of silibinin, including a recently reported meaningful central nervous system activity against brain metastases.

Thematic Areas: Zootecnia / recursos pesqueiros Spectroscopy Saúde coletiva Química Psicología Physical and theoretical chemistry Organic chemistry Odontología Nutrição Molecular biology Medicine (miscellaneous) Medicina veterinaria Medicina iii Medicina ii Medicina i Materiais Interdisciplinar Inorganic chemistry Geociências Farmacia Engenharias iv Engenharias ii Engenharias i Educação física Computer science applications Ciências biológicas iii Ciências biológicas ii Ciências biológicas i Ciências ambientais Ciências agrárias i Ciência de alimentos Ciência da computação Chemistry, multidisciplinary Catalysis Biotecnología Biodiversidade Biochemistry & molecular biology Astronomia / física

licence for use: https://creativecommons.org/licenses/by/3.0/es/

ISSN: 14220067

Author's mail: jorge.joven@urv.cat

Author identifier: 0000-0003-2749-4541

Record's date: 2023-02-18

Papper version: info:eu-repo/semantics/publishedVersion

Link to the original source: https://www.mdpi.com/1422-0067/20/7/1606

Licence document URL: http://repositori.urv.cat/ca/proteccio-de-dades/

Papper original source: International Journal Of Molecular Sciences. 20 (7):

APA: Pérez-Sánchez A; Cuyàs E; Ruiz-Torres V; Agulló-Chazarra L; Verdura S; González-álvarez I; Bermejo M; Joven J; Micol V; Bosch-Barrera J; Menendez J (2019). Intestinal permeability study of clinically relevant formulations of silibinin in caco-2 cell monolayers. International Journal Of Molecular Sciences, 20(7), -. DOI: 10.3390/ijms20071606

Article's DOI: 10.3390/ijms20071606

Entity: Universitat Rovira i Virgili

Journal publication year: 2019

Publication Type: Journal Publications