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Melt-Extruded Microparticles Based On Chitosan-pectin Complex for Delayed Dissolution of Benznidazole
María Sol Magi1,2, Mónica Cristina García1,2, Alvaro Federico Jimenez-Kairuz3,4
1Universidad Nacional de Córdoba (UNC), Facultad de Ciencias Químicas, Departamento de Ciencias Farmacéuticas, Ciudad Universitaria, Haya de La Torre and Medina Allende, Science Building 2, X5000HUA, Córdoba, Argentina.
AAPS Pharmscitech
|December 4, 2025
Summary
This study developed novel interpolyelectrolyte complex (IPEC) microparticles for benznidazole (BNZ) to treat Chagas disease. The new formulation enhances BNZ efficacy and reduces side effects, offering a better therapeutic option.
Area of Science:
- Pharmaceutical Sciences
- Biomaterials Science
- Parasitology
Background:
- Developing well-tolerated drug formulations is crucial for effective treatment delivery.
- Benznidazole (BNZ) is effective for Chagas disease but causes significant side effects, impacting patient adherence.
- Polysaccharide-based biopolymers offer a sustainable and biocompatible basis for advanced drug delivery systems.
Purpose of the Study:
- To design and develop solvent-free interpolyelectrolyte complex (IPEC) microparticles loaded with benznidazole (BNZ).
- To evaluate the potential of these IPEC microparticles as a therapeutic alternative for Chagas disease treatment.
- To assess the impact of the IPEC formulation on BNZ's solubility, release profile, antiparasitic activity, and cytotoxicity.
Main Methods:
- Utilized a melt extrusion technique without organic solvents to create BNZ-loaded IPEC microparticles.
- Incorporated polyethylene glycol to aid polymer processing and high-yield microparticle production.
- Characterized microparticle properties including BNZ distribution, flowability, and mucoadhesion; assessed dissolution and in vitro antiparasitic and cytotoxic effects.
Main Results:
- Achieved high-yield, solvent-free production of BNZ-loaded IPEC microparticles with excellent flow properties.
- Reduced BNZ crystallinity, leading to homogeneous distribution and enhanced solubility in simulated gastric fluid.
- Demonstrated delayed BNZ dissolution, mucoadhesive properties, improved antiparasitic activity against Trypanosoma cruzi, and reduced cytotoxicity in human endothelial cells.
Conclusions:
- Developed a scalable, biocompatible IPEC microparticle platform for benznidazole delivery.
- This formulation offers a promising strategy to optimize Chagas disease treatment by potentially minimizing side effects.
- The IPEC system enhances BNZ's therapeutic profile, suggesting improved patient adherence and treatment outcomes.
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