title: Improvement of Oral Bioavailability of Curcumin upon Microencapsulation with Methacrylic Copolymers.
abstract: 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 investigatedin vitro, ex vivo, andin vivo, and results were compared by laser confocal microscopy analysis. The permeation of microencapsulated CUR through CaCo-2 monolayers was evaluatedin vitro. The mucoadhesion and bioadhesion of the CUR-loaded microparticles were evaluatedin vitro, using E12 and CaCo-2 human intestinal cells, andex 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 theTmaxand a five-fold plasma concentration peak increase.
authors.affiliation: Department of Experimental and Clinical Medicine, University of Catanzaro "Magna Græcia"Catanzaro, Italy; Interregional Research Center for Food Safety and Health, University of Catanzaro "Magna Græcia"Catanzaro, Italy.
authors.forename: Donatella
authors.initials: D
authors.lastname: Paolino
authors.affiliation: Department of Health Sciences, University of Catanzaro "Magna Græcia" Catanzaro, Italy.
authors.forename: Ada
authors.initials: A
authors.lastname: Vero
authors.affiliation: Department of Health Sciences, University of Catanzaro "Magna Græcia" Catanzaro, Italy.
authors.forename: Donato
authors.initials: D
authors.lastname: Cosco
authors.affiliation: Department of Health Sciences, University of Catanzaro "Magna Græcia" Catanzaro, Italy.
authors.forename: Tiziana M G
authors.initials: TM
authors.lastname: Pecora
authors.affiliation: Section of Pharmaceutical Technology, Department of Drug Sciences, University of Catania Catania, Italy.
authors.forename: Simona
authors.initials: S
authors.lastname: Cianciolo
authors.affiliation: Department of Health Sciences, University of Catanzaro "Magna Græcia" Catanzaro, Italy.
authors.forename: Massimo
authors.initials: M
authors.lastname: Fresta
authors.affiliation: Section of Pharmaceutical Technology, Department of Drug Sciences, University of Catania Catania, Italy.
authors.forename: Rosario
authors.initials: R
authors.lastname: Pignatello
keywords: CLSM; CaCo-2 cells; E12 cells; Eudragit®; Retard; microparticles; mucoadhesion