Poster Presenter

Preparation, characterization and in vitro intestinal permeability evaluation of thalidomide inclusion complexes
Cláudia Maria Oliveira Simões, Jadel Kratz, Marina Teixeira, Karine Ferronato, Miguel Caro, Helder Teixeira and Letícia Koester
Brasil

In Brazil, thalidomide (TD) has its distribution restricted to governmental health programs for the treatment of erythema nodosum leprosum, aphthous ulcerations in patients with AIDS, chronic degenerative diseases and multiple myeloma. Although various studies address new clinical applications, the results are inconclusive. A major point that might be implicated in the results variability is its poor aqueous solubility, which led to an erratic and incomplete absorption. This work reports the preparation and characterization of TD-cyclodextrin inclusion complexes, and the effect study of complexation on aqueous solubility, dissolution rate and intestinal permeability of TD. Our results showed that the complexation of TD with hydroxypropyl-β-cyclodextrin (HPβCD) by the kneading technique has improved aqueous solubility and dissolution rate of TD through the enhancement of hydrophilicity and reduction of cristallinity, both resulting from the formation of stable inclusion complexes in the solid state. Additionally, it was demonstrated that TD was able to dissociate from the complexes and permeate across intestinal epithelial Caco-2 cells, with a high permeability profile, equivalent to the free drug. These findings suggest that the TD-HPβCD complex could improve the bioavailability of orally administered TD through the enhancement of its solubility and dissolution, but not through the influence on its permeability.