Di- and Tri-sialo ganglioside micelles load four times more paclitaxel than GM1 monosialoganglioside

HEREDIA V; ALASINO RV; LEONHARD V; BIANCO ID; GARRO AG; BELTRAMO DM

Rosario

Congreso; L Reunión de la Sociedad Argentina de Investigación Bioquímica y Biología Molecular; 2014

Objetives: Characterize self- aggregate structures of ganglioside with two (GD) or three (GT) sialic acid for Ptx and Dox vehiculization and compare the results with those previously described with GM1 micelles. Methods: HPLC, UV-Vis spectrometry, DLS, EM were used to characterize water-solubility and structure. Hep-2 and HeLa cell cultures were used to assess cytotoxicity. Results: The incorporation of drugs at room temperature for both, GD1 and GT1b, complexes achieves an optimum at a molar ratio of 5/1 and were stable in solution for at least 3 months. This stability is also observed upon freeze-thawing, lyophilization-solubilization cycles and high stress condition. GD1 and GT1 micelles showed a size and shape similar to those of GM1. However, contrary to what happens with GM1, the temperature does not change the effectiveness of load of di and tri sialo gangliosides. Finally, in vitro biological activity of the drug contained in GD1 and GT1 micelles was qualitatively equivalent to that of free drug. Conclusion: GD1 and GT1 load four times more Ptx than GM1 micelles. Complexes thus formed are stable and does not affect the biological antimytotic activity of Ptx. These self-assembled nanostructures are new options as drug vehiculization systems.