Cationic liposomes to delivery natural and synthetic compounds for treatment of tumor cells
Maria CONDELLO (Istituto Superiore di Sanità)
ABSTRACT
To improve the therapy of multidrug resistant tumors, we studied new in vitro strategies based on the use of cationic liposomes to delivery antitumor compounds.
Voacamine, a bisindolic alkaloid isolated from Peschiera fuchsifoliae, enhanced the cytotoxic effect of doxorubicin on multidrug resistant tumor cells (Condello et al., 2014). The amine functions of Voacamine were exploited to load it with a high efficacy in the internal aqueous compartment of cationic liposomes, formulated with DOPC, a cationic gemini amphiphilic and cholesterol, by a transmembrane pH gradient. Experiments on osteosarcoma resistant cell line, U-2 OS/DX, showed that Voacamine delivered by liposomes is more efficient than the free alkaloid to revert resistance of cells to doxorubicin.
This liposome formulation was also used to delivery three new 5-Fluorouracil compounds. The cytotoxicity of the formulations was evaluated by MTT assay on HCT116 colon cancer cells. The investigated liposome formulations showed a higher cytotoxicity compared to the free drug, thus showing a great potential in cancer therapy.
