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.

Enhancing the Antitumor Activity of Berberine Hydrochloride by Solid Lipid Nanoparticle Encapsulation

“…Besides, pilot studies in evaluation of the antitumor effect of BH demonstrated that this compound could inhibit proliferation of cancer cells, induce cell cycle at G1/G0 phase, and induce apoptosis in cancer cells (11,12). However, further development and application of this compound has encountered several challenges, particularly in vivo, largely due to its poor aqueous solubility, low gastro-intestinal absorption, and rapid metabolism (13,14). A potential solution to these obstacles is to utilize nanoparticulate formulations, which have been demonstrated to enhance bioavailability and efficacies of loaded water-insoluble drugs (15).…”

Novel Nanostructured Solid Materials for Modulating Oral Drug Delivery from Solid-State Lipid-Based Drug Delivery Systems

“…As might be expected, the majority of published studies have investigated the loading and release of cationic drug molecules from montmorillonite clay (58)(59)(60). Although much less common, anionic drug molecules may also be adsorbed onto montmorillonite, as the edges of the clay sheets carry a slight positive charge due to lattice discontinuities (87).…”

“…Enhanced dissolution and oral bioavailability have been demonstrated for various poorly water-soluble drugs loaded into montmorillonite (58)(59)(60). However, perhaps the most significant limitation of montmorillonite is its propensity to cause incomplete drug release, as demonstrated by Joshi et al (58).…”

“…larger polymeric materials) in montmorillonite delivery systems to allow maximum drug release and bioavailability to be obtained. For example, Oh et al included the cationic polymer polyvinylacetal diethylaminoacetate in montmorillonite-aripiprazole complexes, which acted to enlarge the interlayer spaces of montmorillonite and also facilitated drug release by exchanging with the smaller aripiprazole molecules in vivo (59).…”

Removal of Cyanobacteria <I>Anabaena flos-aquae</I> Through Montmorillonite Clays

“…[1][2][3] Among various clay minerals, the montmorillonite (MMT) clays have been extensively studied in the viewpoint of adsorption materials, especially for removing biological, organic, and inorganic pollutants from drinking water thanks to their large surface area, chemical and mechanical stability, high cation exchange capacity, high absorbing efficiency, biocompatibility and non-toxicity, and low cost. [4][5][6][7][8][9] On the other hand, harmful algal blooms along with eutrophication have been occurring more frequently all over the world, including Republic of Korea. 10 11 The excessive growth of dominant cyanobacteria species involving Microcystis, Oscillatoria, and Anabaena in lakes and rivers not only seriously deteriorate aquatic eco-environment but also threaten water supplies due to the neurotoxin and the hepatotoxin released from them.…”