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Aripiprazole-montmorillonite: A new organic-inorganic nanohybrid material for biomedical applications

Aripiprazole-montmorillonite: A new organic-inorganic nanohybrid material for biomedical applications
Oh Y.-J.Choi G.Choy Y.B.Park J.W.Park J.H.Lee H.J.Yoon Y.J.Chang H.C.Choy J.-H.
Ewha Authors
이화정scopus; 윤여준scopus; 최진호scopus
Issue Date
Journal Title
Chemistry - A European Journal
0947-6539JCR Link
Chemistry - A European Journal vol. 19, no. 15, pp. 4869 - 4875
Document Type
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. Please release me: From an in vitro release study, the drug-release fraction for the AEA-coated aripiprazole-montmorillonite (APZ-MMT) hybrid material was determined to be enhanced up to about 95 % in simulated gastric solution (see figure; AEA=polyvinylacetal diethylamino acetate). Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
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