Eudragit S100 Entrapped Liposome for Curcumin Delivery: Anti-Oxidative Effect in Caco-2 Cells

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.

From waste to health: sustainable exploitation of grape pomace seed extract to manufacture antioxidant, regenerative and prebiotic nanovesicles within circular economy

“…Indeed, recent studies underlined that the incorporation of phytocomplexes in ad hoc modified phospholipid vesicles, can improve their local efficacy in vivo 69 . Recently, De Leo et al 70 incorporated curcumin in eudragit-coated liposomes to create a gastro-resistant carrier, able to protect the payload and deliver it in the colon. Hasibi et al 71 formulated transfersomes containing Tween 80 or Span 60 and confirmed their ability to slowly release taxifolin at intestinal level without evaluating their stability at acidic pH.…”

Recent Advancements in Polymer/Liposome Assembly for Drug Delivery: From Surface Modifications to Hybrid Vesicles

“…Curcumin-loaded liposomes displayed the same antioxidant activity of free curcumin in ethanol, a negligible antioxidant activity when covered with the polymer, which reversed to the normal one after polymer removal. In a subsequent work [ 19 ], the uptake by Caco-2 cells of vesicles loaded with curcumin and coated with Eudragit S100 was assessed. At pH > 7.0, the Eudragit S-100 coating dissolves, releasing the nanometric liposomes and allowing them to enter Caco-2 cells.…”

Concerning Synthesis of New Biobased Polycarbonates with Curcumin in Replacement of Bisphenol A and Recycled Diphenyl Carbonate as Example of Circular Economy

“…Numerous beneficial properties are recognized to this molecule, since many studies have confirmed its antioxidant, anti-inflammatory, antibacterial, and even anti-cancer properties. In order to increase CM water solubility, thus improving its stability and bioavailability, several strategies have been adopted, the main one being the inclusion in liposomes, micelles, solid lipid nanoparticles and in general in polymolecular aggregates of lipids, surfactants, and biopolymers, often in combination with each other [ 14 , 15 , 16 ].…”

“…Numerous beneficial properties are recognized to this molecule, since many studies have confirmed its antioxidant, anti-inflammatory, antibacterial, and even anti-cancer properties. In order to increase CM water solubility, thus improving its stability and bioavailability, several strategies have been adopted, the main one being the inclusion in liposomes, micelles, solid lipid nanoparticles and in general in polymolecular aggregates of lipids, surfactants, and biopolymers, often in combination with each other [14][15][16]. In addition, because of its properties, CM has often been incorporated, functionalized, and conjugated to polymers as a dye, to improve the usability of CM in the field of drug delivery, or to obtain antibacterial, anticancer, and anti-inflammatory biocompatible materials [17][18][19][20].…”