Morphological and physicochemical characterization of liposomes loading cucurbitacin E, an anti-proliferative natural tetracyclic triterpene.

Cucurbitacin E (Cuc E), an oxygenated triterpene molecule, has demonstrated anti-proliferative effect on various cancer cells. Here, we examined the effect of Cuc E on the membrane morphology and properties using differential scanning calorimetry, transmission electron microscopy and atomic force microscopy techniques. Dipalmitoylphosphatidylcholine vesicles were prepared by the thin film hydration method in the absence and presence of Cuc E at molar ratios 100:12 and 100:20. The loading efficiency of Cuc E was found to be higher than 98% upon HPLC analysis. The thermodynamic parameters suggest that Cuc E does not penetrate into the bilayers and interacts with the polar/apolar interface of the lipid membranes. Blank and Cuc E loaded liposomes prepared from a mixture of DPPC/DPPE/DPPG/Cho were imaged by TEM and AFM. Images obtained by TEM revealed unilamellar liposomes for blank and Cuc E loaded liposomes. AFM images showed that the size and the height of Cuc E loaded liposomes were respectively smaller and higher than blank ones. Results suggest that Cuc E produces modifications in the lipid membrane structures.