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Open AccessArticle

Solid Nanocrystals of Rebamipide Promote Recovery from Indomethacin-Induced Gastrointestinal Bleeding

1
Faculty of Pharmacy, Kindai University, 3-4-1 Kowakae, Higashi-Osaka, Osaka 577-8502, Japan
2
Faculty of Pharmaceutical Sciences, Tokushima Bunri University, 180 Yamashiro-Cho, Tokushima 770-8514, Japan
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2019, 20(20), 4990; https://doi.org/10.3390/ijms20204990
Received: 24 September 2019 / Revised: 8 October 2019 / Accepted: 8 October 2019 / Published: 9 October 2019
(This article belongs to the Special Issue Cell-Biomaterial Interaction 2019)
Indomethacin (IMC)-induced gastrointestinal (GI) injuries are more common in rheumatoid arthritis (RA) patients than in other IMC users, and the overexpression of nitric oxide (NO) via inducible NO synthase (iNOS) is related to the seriousness of IMC-induced GI injuries. However, sufficient strategies to prevent IMC-induced GI injuries have not yet been established. In this study, we designed dispersions of rebamipide (RBM) solid nanocrystals (particle size: 30–190 nm) by a bead mill method (RBM-NDs), and investigated whether the oral administration of RBM-NDs is useful to prevent IMC-induced GI injuries. The RBM nanocrystals were spherical and had a solubility 4.71-fold greater than dispersions of traditional RBM powder (RBM-TDs). In addition, the RBM-NDs were stable for 1 month after preparation. The RBM contents in the stomach, jejunum, and ileum of rats orally administered RBM-NDs were significantly higher than in rats administered RBM-TDs. Moreover, the oral administration of RBM-NDs decreased the NO levels via iNOS and area of the GI lesions in IMC-stimulated RA (adjuvant-induced arthritis rat) rats in comparison with the oral administration of RBM-TDs. Thus, we show that the oral administration of RBM-NDs provides a high drug supply to the GI mucosa, resulting in a therapeutic effect on IMC-induced GI injuries. Solid nanocrystalline RBM preparations may offer effective therapy for RA patients. View Full-Text
Keywords: gastrointestinal injury; nanoparticle; rebamipide; indomethacin; rheumatoid arthritis gastrointestinal injury; nanoparticle; rebamipide; indomethacin; rheumatoid arthritis
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MDPI and ACS Style

Nagai, N.; Sakamoto, R.; Yamamoto, S.; Deguchi, S.; Otake, H.; Tanino, T. Solid Nanocrystals of Rebamipide Promote Recovery from Indomethacin-Induced Gastrointestinal Bleeding. Int. J. Mol. Sci. 2019, 20, 4990.

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