Abstract

Natural antioxidants show many pharmacological properties, but poor solubility and inability to cross cell membrane. Liposomes are biocompatible and phospholipid vesicles able to carry hydrophilic, hydrophobic, and amphiphilic molecules. This paper focus on the synthesis of anionic, cationic and zwitterionic liposomes, loaded with quercetin or rutin, and on the evaluation of their cytotoxicity and protective effects against oxidative stress.Chemical characterization was obtained by dynamic light scattering and z-potential experiments. In vitro cell behavior was evaluated by Neutral Red Uptake test.All liposomes, empty and loaded with antioxidants, are stable. The cytotoxicity of both quercetin and rutin encapsulated in zwitterionic and anionic liposomes is higher than that of their solutions. Quercetin and rutin loaded in cationic liposomes are able to inhibit the toxic effect of empty liposomes. The encapsulation of rutin at 5.0×10−5 and 5.0×10−4M, in zwitterionic and anionic liposomes, protects fibroblasts by H2O2 treatment, while the loading with quercetin does not have effect on improving cell viability.All data suggest that the tested liposomes are stable and able to include quercetin and rutin. The liposomes encapsulation of antioxidants makes easier their internalization by cells. Moreover, zwitterionic and anionic liposomes loaded with rutin protect cells by oxidative stress. Liposomes stability together with their good in vitro cytocompatibility, both empty and loaded with antioxidant molecules, makes these systems suitable candidates as drug delivery systems. Moreover, the encapsulation of rutin, is able to protect cells by oxidative stress.

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