Improvement of Oral Bioavailability of Curcumin upon Microencapsulation with Methacrylic Copolymers

Curcumin (diferuloymethane; CUR) is a yellow pigment used in traditional medicine throughout history for its anti-inflammatory activity. In the last years, the scientific research has demonstrated that CUR effects are related to the modulation of crucial molecular targets, related to several patholo...

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Main Authors:	Paolino, Donatella, Vero, Ada, Cosco, Donato, Pecora, Tiziana M. G., Cianciolo, Simona, Fresta, Massimo, Pignatello, Rosario
Format:	Online
Language:	English
Published:	Frontiers Media S.A. 2016
Online Access:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5174134/

id	pubmed-5174134
recordtype	oai_dc
spelling	pubmed-51741342017-01-06 Improvement of Oral Bioavailability of Curcumin upon Microencapsulation with Methacrylic Copolymers Paolino, Donatella Vero, Ada Cosco, Donato Pecora, Tiziana M. G. Cianciolo, Simona Fresta, Massimo Pignatello, Rosario Pharmacology Curcumin (diferuloymethane; CUR) is a yellow pigment used in traditional medicine throughout history for its anti-inflammatory activity. In the last years, the scientific research has demonstrated that CUR effects are related to the modulation of crucial molecular targets, related to several pathologies including cancer, arthritis, diabetes, Crohn’s disease. In this paper, two formulations of microencapsulated CUR obtained by coevaporation with polymethacrylate polymers (Eudragit® Retard) were investigated in vitro, ex vivo, and in vivo, and results were compared by laser confocal microscopy analysis. The permeation of microencapsulated CUR through CaCo-2 monolayers was evaluated in vitro. The mucoadhesion and bioadhesion of the CUR-loaded microparticles were evaluated in vitro, using E12 and CaCo-2 human intestinal cells, and ex vivo, by means of excised rat intestinal mucosa. After oral administration to rats, microencapsulated CUR showed a sevenfold increase of bioavailability in respect to the neat drug, with a concomitant reduction of the Tmax and a five-fold plasma concentration peak increase. Frontiers Media S.A. 2016-12-21 /pmc/articles/PMC5174134/ /pubmed/28066239 http://dx.doi.org/10.3389/fphar.2016.00485 Text en Copyright © 2016 Paolino, Vero, Cosco, Pecora, Cianciolo, Fresta and Pignatello. http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
repository_type	Open Access Journal
institution_category	Foreign Institution
institution	US National Center for Biotechnology Information
building	NCBI PubMed
collection	Online Access
language	English
format	Online
author	Paolino, Donatella Vero, Ada Cosco, Donato Pecora, Tiziana M. G. Cianciolo, Simona Fresta, Massimo Pignatello, Rosario
spellingShingle	Paolino, Donatella Vero, Ada Cosco, Donato Pecora, Tiziana M. G. Cianciolo, Simona Fresta, Massimo Pignatello, Rosario Improvement of Oral Bioavailability of Curcumin upon Microencapsulation with Methacrylic Copolymers
author_facet	Paolino, Donatella Vero, Ada Cosco, Donato Pecora, Tiziana M. G. Cianciolo, Simona Fresta, Massimo Pignatello, Rosario
author_sort	Paolino, Donatella
title	Improvement of Oral Bioavailability of Curcumin upon Microencapsulation with Methacrylic Copolymers
title_short	Improvement of Oral Bioavailability of Curcumin upon Microencapsulation with Methacrylic Copolymers
title_full	Improvement of Oral Bioavailability of Curcumin upon Microencapsulation with Methacrylic Copolymers
title_fullStr	Improvement of Oral Bioavailability of Curcumin upon Microencapsulation with Methacrylic Copolymers
title_full_unstemmed	Improvement of Oral Bioavailability of Curcumin upon Microencapsulation with Methacrylic Copolymers
title_sort	improvement of oral bioavailability of curcumin upon microencapsulation with methacrylic copolymers
description	Curcumin (diferuloymethane; CUR) is a yellow pigment used in traditional medicine throughout history for its anti-inflammatory activity. In the last years, the scientific research has demonstrated that CUR effects are related to the modulation of crucial molecular targets, related to several pathologies including cancer, arthritis, diabetes, Crohn’s disease. In this paper, two formulations of microencapsulated CUR obtained by coevaporation with polymethacrylate polymers (Eudragit® Retard) were investigated in vitro, ex vivo, and in vivo, and results were compared by laser confocal microscopy analysis. The permeation of microencapsulated CUR through CaCo-2 monolayers was evaluated in vitro. The mucoadhesion and bioadhesion of the CUR-loaded microparticles were evaluated in vitro, using E12 and CaCo-2 human intestinal cells, and ex vivo, by means of excised rat intestinal mucosa. After oral administration to rats, microencapsulated CUR showed a sevenfold increase of bioavailability in respect to the neat drug, with a concomitant reduction of the Tmax and a five-fold plasma concentration peak increase.
publisher	Frontiers Media S.A.
publishDate	2016
url	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5174134/
_version_	1613805857553776640

Improvement of Oral Bioavailability of Curcumin upon Microencapsulation with Methacrylic Copolymers

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