DEVELOPMENT OF PEDIATRIC LIQUID DOSAGE FORMS OF BENZNIDAZOLE FOR CHAGAS DISEASE. IN VITRO/IN VIVO STUDIES

SALOMÓN CLAUDIO; LAMAS MARÍA CELINA; MANARIN ROMINA; BOTTASSO EMANUEL; SERRA ESTEBAN; REVELLI SILVIA.

Barcelona, España

Congreso; 6th World Meeting on Pharmaceutics, biopharmaceutics and Pharmaceutical Technology; 2008

Chagas’ disease, a protozoan infection caused by Tripanosoma cruzi, constitutes a major public health problem for developing nations. Congenital transmission has become more relevant as a consequence of the advances in the control of vectorial transmission. In this sense, some countries have specific strategies to deal with this kind of transmission. According to the World Health Organization, 18 to 20 million people in South and Central America and 50,000–100,000 in the United State are infected with Trypanosoma (Schizotrypanum) cruzi, while nearly 90 million persons live in zones where Chagas disease is endemic. Recent surveys indicate that there are 200,000 new cases and 21,000 deaths associated with this condition every year. In addition, approximately 2.800.000 would be children or babiesand another 40 million are at risk of acquiring the disease. In Latin America, the morbidity and mortality associated with Chagas’ disease are more than one order of magnitude higher than those caused by malaria, schistosomiasis or leishmaniasis. One of the drugs most frequently used for the treatment of Chagas disease is Benznidazole (BZL) (1), available only in one fixed dose (tablet of 100 mg). Despite of it is the only treatment for Chagas, it is not adequate for most of the pediatric population. In this context, a research priority should be the development of alternative dosage forms with flexible doses and therefore adaptable to the various weights of children treated.Three vehicles were selected to prepare the liquid dosage forms, focusing in the best solubility parameters, and low solvent toxicity.first time the development of a safe and effective liquid delivery system of BZL (1). Also, this study indicated that liquid formulation of BZLexhibits an important trypanocidal activity in vitro/in vivo in a mousemodel. This is the first demonstration of anti-T. cruzi activity for thistype of formulations. Our results are stimulating enough to continue the development of other liquid dosage forms of BZL (1) as a possible treatment for Chagas disease, particularly in pediatric patients.