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Understanding the Solid Forms of 5 E - phenylethenylbenzofuroxan with Different in vivo anti - T. cruzi Activity [Compreendendo as Formas Sólidas de 5 E - (feniletenil)benzofuroxano com Diferente Atividade anti - T. cruzi in vivo]

Author(s): Sara B. Honorato | Williams Porcal | Alicia Merlino | Javier Ellena | Hugo Cerecetto | Alejandro P. Ayala | Mercedes González

Journal: Revista Virtual de Química
ISSN 1984-6835

Volume: 5;
Issue: 6;
Start page: 1179;
Date: 2013;
Original page

Keywords: Solid forms | 5 E - Phenylethenylbenzofuroxan | anti - T. cruzi agents | solubility | bioavailability

5E-Phenylethenylbenzofuroxan (5PhEBfx) was reported as an excellent anti-Chagas drug candidate.However, its oral bioavailability was affected by the crystallization process. Two samples exhibitingvariable in vivo activity was investigated: a thin yellow powder (5PhEBfx-Y) and orange needles(5PhEBfx-O). X-ray powder diffraction, differential scanning calorimetry, vibrational spectroscopy, optical and electron scanning microscopies were applied to investigate both solid forms in order to correlate the solid-state properties with the variable bioavailability of5PhEBfx. It was observed that 5PhEBfx-Y have a better solubility and consequently higher bioavailability when compared with 5PhEBfx-O. This result suggests that the difference of activity between these two 5E- Phenylethenylbenzofuroxanes could be associated with the solid forms, which also cause the colorationvariation.
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