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Aripiprazole[BOND]Montmorillonite: A New Organic–Inorganic Nanohybrid Material for Biomedical Applications

Authors

  • Yeon-Ji Oh,

    1. Center for Intelligent Nano-Bio Materials (CINBM), Department of Bioinspired Science and Department of Chemistry and Nano Science (Ewha Global Top 5 program), Ewha Womans University, Seoul 120-750 (Korea), Fax: (+82) 2-3277-4340
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  • Goeun Choi,

    1. Center for Intelligent Nano-Bio Materials (CINBM), Department of Bioinspired Science and Department of Chemistry and Nano Science (Ewha Global Top 5 program), Ewha Womans University, Seoul 120-750 (Korea), Fax: (+82) 2-3277-4340
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  • Prof. Young Bin Choy,

    1. Department of Biomedical Engineering, College of Medicine and Institute of Medical and Biological Engineering, Medical Research Center, Seoul National University, Seoul 110-799 (Korea)
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  • Dr. Je Won Park,

    1. Department of Chemistry and Nano Science, Ewha Womans University, Seoul 120-750 (Korea)
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  • Jung Hyun Park,

    1. Division of Life and Pharmaceutical Sciences and College of Pharmacy, Ewha Womans University, Seoul 120-750 (Korea)
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  • Prof. Hwa Jeong Lee,

    1. Division of Life and Pharmaceutical Sciences and College of Pharmacy, Ewha Womans University, Seoul 120-750 (Korea)
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  • Prof. Yeo Joon Yoon,

    1. Department of Chemistry and Nano Science, Ewha Womans University, Seoul 120-750 (Korea)
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  • Hee Chul Chang,

    1. Global Strategy Center and Pharmaceutical Research Institute, Daewoong Pharmaceutical Co., LTD. 135-090, Seoul (Korea)
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  • Prof. Jin-Ho Choy

    Corresponding author
    1. Center for Intelligent Nano-Bio Materials (CINBM), Department of Bioinspired Science and Department of Chemistry and Nano Science (Ewha Global Top 5 program), Ewha Womans University, Seoul 120-750 (Korea), Fax: (+82) 2-3277-4340
    • Center for Intelligent Nano-Bio Materials (CINBM), Department of Bioinspired Science and Department of Chemistry and Nano Science (Ewha Global Top 5 program), Ewha Womans University, Seoul 120-750 (Korea), Fax: (+82) 2-3277-4340
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Abstract

Poor aqueous solubility and the unpleasant taste of aripiprazole (APZ) have been recurring problems, owing to its low bioavailability and low patient tolerance, respectively. Herein, we prepared a nanohybrid system that was based on a bentonite clay material, montmorillonite (MMT), which could both mask the taste and enhance the solubility of APZ (i.e., APZ-MMT). To further improve the efficacy of this taste masking and drug solubility, APZ-MMT was also coated with a cationic polymer, polyvinylacetal diethylamino acetate (AEA). In vitro dissolution tests at neutral pH showed that the amount of drug that was released from the AEA-coated APZ-MMT was greatly suppressed (<1 %) for the first 3 min, thus suggesting that AEA-coated APZ-MMT has strong potential for the taste masking of APZ. Notably, in simulated gastric juice at pH 1.2, the total percentage of APZ that was released within the first 2 h increased up to 95 % for AEA-coated APZ-MMT. Furthermore, this in vitro release profile was also similar to that of Abilify®, a commercially available medication. In vivo experiments by using Sprague–Dawley rats were also performed to compare the pharmacokinetics of AEA-coated APZ-MMT and Abilify®. AEA-coated APZ-MMT exhibited about 20 % higher systemic exposure of APZ and its metabolite, dehydro-APZ, compared with Abilify®. Therefore, a new MMT-based nanovehicle, which is coated with a cationic polymer, can act as a promising delivery system for both taste masking and for enhancing the bioavailability of APZ.

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