title: Aripiprazole-montmorillonite: a new organic-inorganic nanohybrid material for biomedical applications.
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.
authors: 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.
authors: Yeon-Ji
authors: YJ
authors: Oh
authors: Goeun
authors: G
authors: Choi
authors: Young Bin
authors: YB
authors: Choy
authors: Je Won
authors: JW
authors: Park
authors: Jung Hyun
authors: JH
authors: Park
authors: Hwa Jeong
authors: HJ
authors: Lee
authors: Yeo Joon
authors: YJ
authors: Yoon
authors: Hee Chul
authors: HC
authors: Chang
authors: Jin-Ho
authors: JH
authors: Choy
mesh_terms: D000818:Animals; D000068180:Aripiprazole; D001546:Bentonite / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D001682:Biological Availability; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008297:Male; D049329:Nanostructures; D010879:Piperazines / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D011108:Polymers / Q000737:chemistry; D015363:Quinolones / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013649:Taste
chemical_list: D010879:Piperazines; D011108:Polymers; D015363:Quinolones; D001546:Bentonite; D000068180:Aripiprazole