Self-assembled micelles of monosialogangliosides as nanodelivery vehicles for taxanes

V. LEONHARD; ALASINO R.V.; BIANCO I.D.; GARRO, A.G.; HEREDIA V.; BELTRAMO D.M.

ELSEVIER SCIENCE BV

Lugar: Amsterdam; Año: 2012 vol. 162 p. 619 - 619

e demonstrate herein that taxanes (paclitaxel (Ptx) and docetaxel (Dtx)) can be spontaneously loaded into ganglioside nanomicelles. The efficiency of gangliosides to solubilize taxanes was highly dependent on their self-aggregating structure. Thus, GM3 that forms unilamellar vesicles was less efficient to solubilize taxanes than gangliosides that form micelles (i.e.: GM1 and GM2). Sialic acid cyclization of GM1 by acid treatment led to an important reduction in its capacity to solubilize taxanes, as also did the replacement of the fatty acid of ceramide by a dicholoracetyl group. Water solubility of paclitaxel (Ptx) is less than 1 µg.mL-1 and increased up to 6.3 mg.mL-1 upon its association with GM1 micelles. The incorporation of Ptx in GM1 reached an optimum at GM1/Ptx 20/1 molar ratio when performed at room temperature. An increase in the solubilization capacity of GM1 micelles was observed upon dehydration of their polar head group by pre-treatment at 55 oC. Loading of Ptx into t