Development of benznidazole orally disintegrating tablets for paediatric patients

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Tropical Medicine

Background:

• American Trypanosomiasis (Chagas disease) is a neglected tropical disease affecting millions, particularly children.
• Current benznidazole (BNZ) formulations lack pediatric-specific preparations, hindering effective treatment in children.
• There is a critical need for improved drug delivery systems for Chagas disease therapy.

Purpose of the Study:

• To develop orally disintegrating tablets (ODTs) of benznidazole (BNZ) for improved Chagas disease treatment.
• To enhance the dissolution rate and bioavailability of BNZ in a pediatric-friendly dosage form.
• To ensure the stability and quality of the developed BNZ ODTs.

Main Methods:

• Co-milling and direct compression were employed to create BNZ ODTs.
• Taste masking and preference studies were conducted with adult volunteers.
• Tablets underwent comprehensive characterization, including stability and bioavailability assessments.

Main Results:

• The developed BNZ ODTs exhibited rapid disintegration (30 seconds) and enhanced dissolution rates.
• BNZ maintained its crystalline form (form I) within the ODTs.
• The ODTs demonstrated stability for at least one year, with comparable oral bioavailability to pulverized commercial tablets.

Conclusions:

• The developed benznidazole orally disintegrating tablets show promise for improving pediatric Chagas disease therapeutics.
• This novel formulation addresses the need for specialized pediatric treatments for Chagas disease.
• The study highlights the potential of ODT technology for neglected disease drug development.