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Albendazole Microcrystal Formulations Based on Chitosan and Cellulose Derivatives: Physicochemical Characterization and In Vitro Parasiticidal Activity in Trichinella spiralis Adult Worms

  • Research Article
  • Theme: Recent Trends in the Development of Chitosan-Based Drug Delivery Systems
  • Published:
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Abstract

The oral route has notable advantages to administering dosage forms. One of the most important questions to solve is the poor solubility of most drugs which produces low bioavailability and delivery problems, a major challenge for the pharmaceutical industry. Albendazole is a benzimidazole carbamate extensively used in oral chemotherapy against intestinal parasites, due to its extended spectrum activity and low cost. Nevertheless, the main disadvantage is the poor bioavailability due to its very low solubility in water. The main objective of this study was to prepare microcrystal formulations by the bottom-up technology to increase albendazole dissolution rate, in order to enhance its antiparasitic activity. Thus, 20 novel microstructures based on chitosan, cellulose derivatives, and poloxamer as a surfactant were produced and characterized by their physicochemical properties and in vitro biological activity. To determine the significance of type and concentration of polymer, and presence or absence of surfactant in the crystals, the variables area under the curve, albendazole microcrystal solubility, and drug released (%) at 30 min were analyzed with a three-way ANOVA. This analysis indicated that the microcrystals made with hydroxyethylcellulose or chitosan appear to be the best options to optimize oral absorption of the active pharmaceutical ingredient. The in vitro evaluation of anthelmintic activity on adult forms of Trichinella spiralis identified system S10A as the most effective, of choice for testing therapeutic efficacy in vivo.

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Acknowledgments

J.P. is grateful to CONICET (Consejo Nacional de Investigaciones Científicas y Técnicas) for a doctoral fellowship. A.V.C is grateful to CIUNR (Consejo de Investigaciones, Universidad Nacional de Rosario) for a research fellowship.

This work was supported by the Universidad Nacional de Rosario, Consejo Nacional de Investigaciones Científicas y Técnicas (Project N° PIP 112-201001-00194) and Agencia Nacional de Promoción Científica y Tecnológica (Project N° PICT 2006-1126).

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    Authors and Affiliations

    1. IQUIR-CONICET, Suipacha 570, 2000, Rosario, Argentina

      Josefina Priotti, Darío Leonardi & María C. Lamas

    2. Instituto de Genética Experimental, Facultad de Ciencias Médicas, Universidad Nacional de Rosario, Santa Fe 3100, S2000KTR, Rosario, Argentina

      Ana V. Codina, María D. Vasconi & Lucila I. Hinrichsen

    3. Departamento de Farmacia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 570, 2000, Rosario, Argentina

      Darío Leonardi & María C. Lamas

    4. Área Parasitología, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 570, 2000, Rosario, Argentina

      María D. Vasconi

    5. CIC-UNR, Universidad Nacional de Rosario, Maipú 1065, 2000, Rosario, Argentina

      Lucila I. Hinrichsen

    6. Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, 2000, Rosario, Argentina

      María C. Lamas

    Authors
    1. Josefina Priotti
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    2. Ana V. Codina
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    3. Darío Leonardi
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    5. Lucila I. Hinrichsen
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    6. María C. Lamas
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    Corresponding authors

    Correspondence to Lucila I. Hinrichsen or María C. Lamas.

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    Guest Editors: Claudio Salomon, Francisco Goycoolea, and Bruno Moerschbacher

    Josefina Priotti and Ana V. Codina contributed equally to this work.

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    Priotti, J., Codina, A.V., Leonardi, D. et al. Albendazole Microcrystal Formulations Based on Chitosan and Cellulose Derivatives: Physicochemical Characterization and In Vitro Parasiticidal Activity in Trichinella spiralis Adult Worms. AAPS PharmSciTech 18, 947–956 (2017). https://doi.org/10.1208/s12249-016-0659-z

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    • DOI: https://doi.org/10.1208/s12249-016-0659-z

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