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Open AccessCommunication

Intestinal Permeability Study of Clinically Relevant Formulations of Silibinin in Caco-2 Cell Monolayers

Instituto de Biología Molecular y Celular (IBMC) and Instituto de Investigación, Desarrollo e Innovación en Biotecnología Sanitaria de Elche (IDiBE), Universidad Miguel Hernández (UMH), 03202 Elche, Spain
Program Against Cancer Therapeutic Resistance (ProCURE), Metabolism and Cancer Group, Catalan Institute of Oncology, 17007 Girona, Spain
Girona Biomedical Research Institute (IDIBGI), 17190 Girona, Spain
Pharmacokinetics and Pharmaceutical Technology Area, Engineering Department, Universidad Miguel Hernández (UMH), San Juan de Alicante, 03202 Alicante, Spain
Unitat de Recerca Biomèdica, Hospital Universitari Sant Joan, Institut d’Investigació Sanitària Pere Virgili, Universitat Rovira i Virgili, 43201 Reus, Spain
CIBER, Fisiopatología de la Obesidad y la Nutrición, CIBERobn, Instituto de Salud Carlos III (CB12/03/30038), 07122 Palma de Mallorca, Spain
Department of Medical Sciences, Medical School University of Girona, 17003 Girona, Spain
Medical Oncology, Catalan Institute of Oncology (ICO), Dr. Josep Trueta University Hospital, 17007 Girona, Spain
Authors to whom correspondence should be addressed.
These authors contributed equally.
Int. J. Mol. Sci. 2019, 20(7), 1606;
Received: 14 March 2019 / Revised: 27 March 2019 / Accepted: 29 March 2019 / Published: 31 March 2019
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. View Full-Text
Keywords: silibinin; cancer; bioavailability; blood–brain barrier silibinin; cancer; bioavailability; blood–brain barrier
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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.A. Intestinal Permeability Study of Clinically Relevant Formulations of Silibinin in Caco-2 Cell Monolayers. Int. J. Mol. Sci. 2019, 20, 1606.

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