Physicochemical characterization of orally-active meglumine antimoniate/beta-cyclodextrin nanoassemblies: non-inclusion interactions and sustained drug release properties

Martins, P. S., Ribeiro, R. R., Bahia, A. P. C, M. Neto, R. L., Frézard, F., Pimenta, A. M. C., Melo, A. L., Le Moyec, L., Demicheli, C.

Physicochemical characterization of orally-active meglumine antimoniate/beta-cyclodextrin nanoassemblies: non-inclusion interactions and sustained drug release properties

AUTOR(ES)

Martins, P. S., Ribeiro, R. R., Bahia, A. P. C, M. Neto, R. L., Frézard, F., Pimenta, A. M. C., Melo, A. L., Le Moyec, L., Demicheli, C.

FONTE

Brazilian Journal of Physics

DATA DE PUBLICAÇÃO

2009-04

RESUMO

β-cyclodextrin (β-CD) is widely used as a component of pharmaceutical formulations, classically to improve the solubility and oral bioavailability of poorly water-soluble drugs through formation of drug/β-CD inclusion complexes. Unexpectedly, the association of the highly water-soluble drug meglumine antimoniate (MA) with β-CD turned this antimonial compound orally-active in a murine model of leishmaniasis. To get insight into the mechanisms responsible for the enhanced oral efficacy of MA, the MA/β-CD composition was characterized physicochemically, using thermogravimetry, circular dichroism, mass spectrometry (ESI-MS), osmometry and photon correlation spectroscopy. The freeze-dried MA/β-CD was found to form nanoassemblies in water, as a result of multiple non-inclusion interactions between MA and β-CD, which behave as a sustained release system of the MA drug.