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Preparation and characterization of liposomes incorporating cucurbitacin E, a natural cytotoxic triterpene

Abstract : Cucurbitacin E (Cuc E), highly oxygenated triterpene from cucurbitaceae ă family, was demonstrated to possess anti-proliferative, ă anti-inflammatory and anti-oxidant activities. Here, we studied the ă effect of Cuc E on the properties of the phospholipid membrane. Large ă unilamellar vesicles, with and without sulforhodamine B (SRB), were ă prepared in the absence and presence of Cuc E. The fluorescence ă increase, resulting from SRB release from vesicles due to inhibition of ă auto-quenching, was used to assess the permeability of liposome at 4 ă degrees and 37 degrees C. At 4 degrees C, blank liposomes and those ă containing Cuc E were stable; while at 37 degrees C Cuc E loaded ă liposomes showed less stability than blank ones. The loading efficiency ă of Cuc E into the vesicles was demonstrated to be 85% by HPLC. Dynamic ă light scattering measurements showed that liposomes embedding Cuc E were ă smaller than those which did not. Multilamellar vesicles were ă manufactured from dipalmitoylphosphatidylcholine in the presence and ă absence of Cuc E (molar ratio 7%). Results obtained by differential ă scanning calorimetry suggest that Cuc E binds mainly at the polar/apolar ă interfacial region of lipid bilayers and may incorporate into the lipid ă bilayer. Cuc E does not produce phase separation and thus might be ă included in liposome formulation. (C) 2013 Elsevier B.V. All rights ă reserved.
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Lamice Habib, Nathalie Khreich, Alia Jraij, Suzanne Abbas, Jacques Magdalou, et al.. Preparation and characterization of liposomes incorporating cucurbitacin E, a natural cytotoxic triterpene. International Journal of Pharmaceutics, Elsevier, 2013, 448 (1), pp.313-319. ⟨10.1016/j.ijpharm.2013.03.027⟩. ⟨hal-01464670⟩



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