Abstract
Curcumin is a natural polyphenol with strong antioxidant activity. However, this molecule shows a very poor bioavailability, instability, and rapid metabolism in vivo. In this work curcumin was loaded in Eudragit-coated liposomes to create a gastroresistant carrier, able to protect its load from degradation and free it at the site of absorption in the colon region. Small unilamellar vesicles were prepared and coated with Eudragit by a pH-driven method. The physico-chemical properties of the prepared systems were assessed by light scattering, transmission electron microscopy, infrared spectroscopy, and differential scanning calorimetry. The uptake of vesicles by Caco-2 cells and the anti-oxidant activity in cells were evaluated. The produced vesicles showed dimensions of about forty nanometers that after covering with Eudragit resulted to have micrometric dimensions at acid pH. The experiments showed that at pH > 7.0 the polymeric coating dissolves, releasing the nanometric liposomes and allowing them to enter Caco-2 cells. Delivered curcumin loaded vesicles were then able to decrease significantly ROS levels as induced by H2O2 in Caco-2 cells. The proposed work showed the possibility of realizing effective gastroresistant curcumin liposome formulations for the delivery of antioxidant molecules to Caco-2 cells, potentially applicable to the treatment of pathological conditions related to intestinal oxidative stress.
Highlights
Curcumin is a natural polyphenol with strong antioxidant activity
Previous studies have shown that liposomes of around 40 nm give rise to a 12-fold higher uptake in Caco-2 cells than vesicles larger than 100 nm [27]
In order to obtain gastro-resistant vesicles, curcumin-loaded liposomes covered with Eudragit®(Eu-Curc-liposome) were obtained according to a recently described method [24], which allows to obtain clusters of vesicles covered with polymer capable of protecting liposomes and their payload from the acid compartments of the gastrointestinal tract
Summary
Curcumin is a natural polyphenol with strong antioxidant activity. this molecule shows a very poor bioavailability, instability, and rapid metabolism in vivo. The proposed work showed the possibility of realizing effective gastroresistant curcumin liposome formulations for the delivery of antioxidant molecules to Caco-2 cells, potentially applicable to the treatment of pathological conditions related to intestinal oxidative stress. The precise mechanism of action of curcumin are still under investigation by researchers, the innumerable therapeutic benefits deriving from curcumin supplementation are mainly attributable to its antioxidant and anti-inflammatory effects [4] This polyphenol and its derivatives showed strong activities against various typologies of cancer by arresting them in various phases of the cell cycle and disease development [5,6]. Liposomes are ideal carriers for curcumin delivery in a wide range of applications, as demonstrated by numerous researchers [14,15,16] They consist of a phospholipid bilayer, fully biocompatible and safe, that encloses an aqueous core. Liposomes can be covered with both natural and synthetic polymers that increase their steric and biological stability, adapting them to specific experimental needs [22,23]
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