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A Novel Prototype Device for Microencapsulation of Benznidazole: In Vitro/In Vivo Studies

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Abstract

This study was aimed to design a simple and novel prototype device for the production of polymeric microparticles. To prove the effectiveness of this device, benznidazole microparticles using chitosan as carrier and NaOH, KOH, or SLS as counter ions were used. For comparison, benznidazole microparticles were prepared by the conventional dripping technique (syringe and gauge) using the same excipients. Microparticles were characterized in terms of encapsulation efficiency, particle shape, size and surface topography, crystallinity characteristics, thermal behavior, and dissolution rate. Then, the pharmacokinetic parameters were evaluated after the oral administration of the microparticles to healthy Wistar rats. The prepared formulations, by means of this device, showed good drug encapsulation efficiency (> 70%). Release studies revealed an increased dissolution of benznidazole from chitosan microparticles prepared using the novel device. It achieved more than 90% in 60 min, while those of the conventional microparticles and raw drug achieved 65% and 68%, respectively, during the same period. Almost spherical benznidazole microparticles with a smooth surface and size around 10–30 μm were observed using scanning electron microscopy. Thermal analysis and X-ray diffraction studies suggested a partial reduction of drug crystallinity. Moreover, the relative oral bioavailability of the novel benznidazole microparticles showed that the area under the curve for the microencapsulated drug was 10.3 times higher than the raw drug. Thus, these findings indicate that the designed glass prototype device is a useful alternative to formulate benznidazole polymeric microparticles with improved biopharmaceutical properties and could be useful for other therapeutic microparticulate systems.

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Funding

The National University of Rosario (UNR) and the National Council Research (CONICET) provided financial support.

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Authors and Affiliations

  1. Departamento Farmacia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, S2002LRK, Rosario, Argentina

    María G. Barrera, Darío Leonardi, María C. Lamas & Claudio J. Salomón

  2. IQUIR – CONICET, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, S2002LRK, Rosario, Argentina

    Guillermo Tejada, Darío Leonardi, María C. Lamas & Claudio J. Salomón

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  1. María G. Barrera
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  2. Guillermo Tejada
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  3. Darío Leonardi
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  4. María C. Lamas
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  5. Claudio J. Salomón
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Correspondence to Claudio J. Salomón.

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This study was authorized by the Ethical Committee on Animal Experimentation of the Faculty of Biochemical and Pharmaceutical Sciences, National University of Rosario (Argentina). Also, experiments with animals were performed according to the ethical standards formulated in the Declaration of Helsinki, and appropriate measures were taken to protect animals from pain or discomfort.

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Barrera, M.G., Tejada, G., Leonardi, D. et al. A Novel Prototype Device for Microencapsulation of Benznidazole: In Vitro/In Vivo Studies. AAPS PharmSciTech 21, 112 (2020). https://doi.org/10.1208/s12249-020-01659-3

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