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 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.
Highlights
Curcumin [1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione; CUR] is the most active component of turmeric (Curcuma longa), a perennial herb belonging to the ginger family
It has been used in traditional Indian medicine for about 6000 years to treat wounds, rheumatism and inflammatory diseases (Corson and Crews, 2007; Jurenka, 2009; Leonti and Casu, 2013) but, in the last 50 years, scientific research demonstrated that CUR possesses additional activities such as antioxidant (Soudamini et al, 1992), anti-inflammatory (Abe et al, 1999), anti-atherosclerotic, anti-angiogenesis, and anti-carcinogenic ones (Kunnumakkara et al, 2008)
We developed CUR-loaded microparticles made up of Eudragit R Retard copolymers, and we observed that this approach, was not effective in improving the solubility of CUR in simulated gastric and intestinal fluids, was instead able to protect the drug from UV light-induced chemical degradation (Pecora et al, 2016)
Summary
Curcumin [1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione; CUR] is the most active component of turmeric (Curcuma longa), a perennial herb belonging to the ginger family. It has been used in traditional Indian medicine for about 6000 years to treat wounds, rheumatism and inflammatory diseases (Corson and Crews, 2007; Jurenka, 2009; Leonti and Casu, 2013) but, in the last 50 years, scientific research demonstrated that CUR possesses additional activities such as antioxidant (Soudamini et al, 1992), anti-inflammatory (Abe et al, 1999), anti-atherosclerotic, anti-angiogenesis, and anti-carcinogenic ones (Kunnumakkara et al, 2008). Many preclinical and clinical studies have confirmed that CUR is significantly non-toxic even at very high doses (Mohanty et al, 2012)
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