Benznidazole-Loaded Polymeric Nanoparticles for Oral Chemotherapeutic Treatment of Chagas Disease

• Published in: Pharmaceutics 2024-06, Vol.16 (6), p.800
• Main Authors: Sousa, Lucas Resende Dutra, Duarte, Thays Helena Chaves, Xavier, Viviane Flores, das Mercês, Aline Coelho, Vieira, Gabriel Maia, Martins, Maximiliano Delany, Carneiro, Cláudia Martins, Dos Santos, Viviane Martins Rebello, Dos Santos, Orlando David Henrique, Vieira, Paula Melo de Abreu
• Format: Article
• Language: English
• Subjects: benznidazole; Chagas disease; Chemical properties; Chemotherapy; Diagnosis; Drug delivery systems; Drug therapy; formulations; Health aspects; Nanoparticles; Oral administration; Patients; Polyethylene glycol; polymeric nanoparticles; Polymers; Polyvinyl alcohol; Scanning electron microscopy; trypanocidal activity
• ISSN: 1999-4923; 1999-4923
• DOI: 10.3390/pharmaceutics16060800

Chagas disease (CD) is a worldwide public health problem. Benznidazole (BZ) is the drug used to treat it. However, in its commercial formulation, it has significant side effects and is less effective in the chronic phase of the infection. The development of particulate systems containing BZ is therefore being promoted. The objective of this investigation was to develop polymeric nanoparticles loaded with BZ and examine their trypanocidal impact in vitro. Two formulas (BNP1 and BNP2) were produced through double emulsification and freeze drying. Subsequent to physicochemical and morphological assessment, both formulations exhibited adequate yield, average particle diameter, and zeta potential for oral administration. Cell viability was assessed in H9C2 and RAW 264.7 cells in vitro, revealing no cytotoxicity in cardiomyocytes or detrimental effects in macrophages at specific concentrations. BNP1 and BNP2 enhanced the effect of BZ within 48 h using a treatment of 3.90 μg/mL. The formulations notably improved NO reduction, particularly BNP2. The findings imply that the compositions are suitable for preclinical research, underscoring their potential as substitutes for treating CD. This study aids the quest for new BZ formulations, which are essential in light of the disregard for the treatment of CD and the unfavorable effects associated with its commercial product.