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Caddeo, C., Gabriele, M., Nácher, A., Fernàndez-Busquets, X., Valenti, D., Maria Fadda, A., Pucci, L., Manconi, M., (2021). Resveratrol and artemisinin eudragit-coated liposomes: A strategy to tackle intestinal tumors International Journal of Pharmaceutics 592

Resveratrol and artemisinin, two naturally occurring compounds with a wide range of biological activities, have been reported to exert antitumor effects against several types of cancer. In this work, Eudragit-coated liposomes were developed to safely transport resveratrol and artemisinin through the gastrointestinal tract and target the intestine. The physico-chemical properties of the Eudragit-coated liposomes were assessed by light scattering and cryogenic transmission electron microscopy. Nanosized (around 100 nm), spherical or elongated, unilamellar vesicles were produced. The protective effect of the Eudragit coating was confirmed by assessing the physical stability of the vesicles in fluids mimicking the gastrointestinal environment. Furthermore, the vesicles were found to exert a pro-oxidant activity in intestinal adenocarcinoma cells, which resulted in a marked mortality due to the generation of reactive oxygen species (ROS). A time- and dose-dependent cell growth inhibitory effect was detected, with elevated ROS levels when resveratrol and artemisinin were combined. Therefore, the proposed formulations may represent a valuable means to counteract intestinal tumor growth. © 2020 Elsevier B.V.

Keywords: Antitumor, Artemisinin, Eudragit, Intestinal delivery, Liposomes, Resveratrol