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Improving Properties of Albendazole Desmotropes by Supramolecular Systems with Maltodextrin and Glutamic Acid

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Abstract

Albendazole, an effective broad-spectrum anthelmintic agent, showed unpredictable therapeutic response caused by poor water solubility and slow dissolution rate. Then, novel binary and multicomponent supramolecular systems of two different solid forms of albendazole (I and II) with maltodextrin alone or with glutamic acid were studied as an alternative to improve the oral bioavailability of albendazole. The interactions and effects on the properties of albendazole were studied in solution and solid state. The solid systems were characterized using Raman and Fourier transform-infrared spectroscopy, thermal analysis, powder X-ray diffraction, and scanning electron microscopy. The solubility measurements, performed in aqueous and simulated gastric fluid, showed that albendazole (form II) was the most soluble form, while its supramolecular systems showed the highest solubility in simulated gastric fluid. On the other hand, the dissolution profiles of binary and multicomponent systems in simulated gastric fluid displayed pronounced increments of the dissolved drug and a faster dissolution rate compared to those of free albendazole forms. Thus, these supramolecular structures constitute an interesting alternative to improve the physicochemical properties of albendazole, with potential application for the preparation of pharmaceutical oral formulations.

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Acknowledgments

Authors wish to acknowledge the assistance of the Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET) and the Universidad Nacional de Córdoba, both of which provided support and facilities for this investigation. Also, project MinCyT-CONICET-CAPES is gratefully acknowledged.

Funding

The authors thank the Fondo para la Investigación Científica y Tecnológica (FONCYT) [Préstamo BID PICT 2013-0504], the Secretaría de Ciencia y Técnica de la Universidad Nacional de Córdoba (SECyT), and the Brazilian National Council for Scientific and Technological Development (CNPQ) for financial support.

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Authors and Affiliations

  1. Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Córdoba, Argentina

    Agustina Bongioanni, Marcela R. Longhi & Claudia Garnero

  2. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica—UNITEFA (CONICET-UNC), Córdoba, Argentina

    Agustina Bongioanni, Marcela R. Longhi & Claudia Garnero

  3. Departamento de Física, Universidade Federal do Ceará, Fortaleza, Ceara, Brazil

    Bruno Sousa Araújo & Alejandro Ayala

  4. Departamento de Farmácia, Universidade Federal do Ceará, Fortaleza, Ceara, Brazil

    Yara Santiago de Oliveira

Authors
  1. Agustina Bongioanni
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  2. Bruno Sousa Araújo
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  3. Yara Santiago de Oliveira
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  4. Marcela R. Longhi
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  5. Alejandro Ayala
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  6. Claudia Garnero
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Corresponding author

Correspondence to Claudia Garnero.

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Bongioanni, A., Araújo, B.S., de Oliveira, Y.S. et al. Improving Properties of Albendazole Desmotropes by Supramolecular Systems with Maltodextrin and Glutamic Acid. AAPS PharmSciTech 19, 1468–1476 (2018). https://doi.org/10.1208/s12249-018-0952-0

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