Comparative Cellular and In Vivo Anticancer Studies of Doxorubicin Liposomes Prepared with Different Types of Phospholipids

Liposomes have been widely used to improve drug accumulation in cancer therapy, enhancing anticancer efficacy and reducing side effects. The lipid components of the bilayer membrane define the fluidity of liposomes, which affects drug effectiveness. The present study evaluated the effectiveness of liposomes of differing rigidity in delivering doxorubicin (DOX). In this study, a phospholipid with a high Tm, hydrogenated soy phosphatidylcholine (HSPC), was totally or partially substituted with1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) or1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE). The liposomes loaded DOX were composed of phosphatidylcholine (HSPC, POPC), both combined and not combined with DOPE, at a molar ratio of total phospholipids: cholesterol and DSPE-mPEG2000 were 57:38:5, respectively, and produced using a thin-layer hydration method. The in vitro cytotoxicity and in vivo antitumor activity of these liposomes was subsequently evaluated. The in vitro cytotoxicity assay used murine Lewis lung cancer (LLC) cells and Colon Carcinoma (C26) cells. For in vivo evaluation, the sample was intravenously injected into mice's tail veins at a dose of 5 mg DOX per kg of body weight. The results showed that substituting HSPC with POPC resulted in cytotoxicity profiles similar to those of DOX solution on C26 colon cancer and LLC cells. The addition of DOPE to DOX liposomes reduced antitumor activity. It can be concluded that the HSPC substituted with POPC or DOPE reduced liposome rigidity while also lowering in vivo antitumor activity.