Evaluation of a new dendrimeric structure as prospective drugs carrier for intravenous administration of antichagasic active compounds

LUCIANA FERNANDEZ; MARCELO CALDERÓN; MARISA MARTINELLI; MIRIAM STRUMIA; HUGO CERECETTO; MERCEDES GONZALEZ; JUANA SILBER; MARISA SANTO

JOURNAL OF PHYSICAL ORGANIC CHEMISTRY

JOHN WILEY & SONS LTD

Año: 2008 p. 1079 - 1085

0894-3230

In the present work, we investigated a first generation of a new dendrimer as candidate for intravenous (iv) administration of a therapeutic compound (2(-(benzo[1,2-c] 1,2,5-oxadiazol-5(6)-yl (N-1-oxide) methylidene]-1- methoxy methane hydrazide). This compound presents antichagasic activity but low water solubility. Guest–host specific interactions results in good drug solubilization. These interactions can be controlled by varying the solution pH, allowing drug deliverance. Interaction between dendrimer and human serum albumin (HSA), and the hemolytic potential of dendrimer were evaluated. The dendrimer does not interact with blood proteins, is not hemolytic, and does not produce damage in the cellular membrane. The results demonstrate that the new dendritic structure could be an appropriate carrier for the novel antichagasic drug(-(benzo[1,2-c] 1,2,5-oxadiazol-5(6)-yl (N-1-oxide) methylidene]-1- methoxy methane hydrazide). This compound presents antichagasic activity but low water solubility. Guest–host specific interactions results in good drug solubilization. These interactions can be controlled by varying the solution pH, allowing drug deliverance. Interaction between dendrimer and human serum albumin (HSA), and the hemolytic potential of dendrimer were evaluated. The dendrimer does not interact with blood proteins, is not hemolytic, and does not produce damage in the cellular membrane. The results demonstrate that the new dendritic structure could be an appropriate carrier for the novel antichagasic drug