Encapsulation of Benznidazole in Polymeric Microparticles for the Treatment of Chagas Disease.

OKULIC C. ; SEREMETA K.; SALOMON C.

Congreso; 2017 AAPS ANUAL MEETING AND EXPOSITION; 2017

AAPS

Benznidazole (BNZ) is the trypanocidal drug of choice for the treatment of Chagas disease. Even though most infections occur during childhood, including newborn babies, to date, BNZ is only available in tablets, a highly inappropriate dosage form for newborns and children. In these cases, such tablets are usually fractioned by hand, which may result in improper dosage increasing the risk of side effects. The high doses of BNZ required and the long treatment (30-60 days) often leads to the development of several adverse effects and noncompliance by the patients. BNZ is poorly soluble in water (0.4 mg/mL) which limits its oral absorption and bioavailability.The aim of this work was to evaluate whether the spray-drying process might be a proper technology for the preparation of BNZ microparticles (BNZ-MPs) with enhanced dissolution rate as a specific paediatric formulation for Chagas disease.The development of novel BNZ polymeric MPs resulted in enhanced drug dissolution compared to the non-encapsulated BNZ. Such formulations proved to be very stable without reduction of drug loading. BNZ-MPs would be a convenient approach for enhancing oral bioavailability and reducing, probably, the dose requirements while minimizing the serious side effects. In addition, these BNZ-MPs formulated into an aqueous suspension would allow dose flexibility to suit the dosing requirements across all age groups.