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Pharmaceutics
Volume 12
Issue 6
10.3390/pharmaceutics12060532
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Article

Hydrogel Formulations Incorporating Drug Nanocrystals Enhance the Therapeutic Effect of Rebamipide in a Hamster Model for Oral Mucositis

by
Noriaki Nagai
1,*,
Ryotaro Seiriki
1,
Saori Deguchi
1,
Hiroko Otake
1,
Noriko Hiramatsu
2,
Hiroshi Sasaki
3 and
Naoki Yamamoto
3
1
Faculty of Pharmacy, Kindai University, 3-4-1 Kowakae, Higashi-Osaka, Osaka 577-8502, Japan
2
Laboratory of Molecularbiology and Histochemistry, Fujita Health University Institute of Joint Research, 1-98 Dengakugakubo, Kutsukake, Toyoake, Aichi 470-1192, Japan
3
Department of Ophthalmology, Kanazawa Medical University, 1-1 Daigaku, Uchinada, Kahoku, Ishikawa 920-0293, Japan
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(6), 532; https://doi.org/10.3390/pharmaceutics12060532
Submission received: 21 May 2020 / Revised: 7 June 2020 / Accepted: 8 June 2020 / Published: 9 June 2020
(This article belongs to the Special Issue Drug Absorption Studies: In Situ, In Vitro and In Silico Models)
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Abstract

A mouthwash formulation of rebamipide (REB) is commonly used to treat oral mucositis; however, this formulation does not provide sufficient treatment or prevention in cases of serious oral mucositis. To improve treatment, we attempted to design a hydrogel incorporating REB nanocrystals (R-NPs gel). The R-NPs gel was prepared by a bead mill method using carbopol hydrogel, methylcellulose and 2-hydroxypropyl-β-cyclodextrin, and another hydrogel incorporating REB microcrystals (R-MPs gel) was prepared following the same protocol but without the bead mill treatment. The REB particle size in the R-MPs gel was 0.15–25 μm, and while the REB particle size was 50–180 nm in the R-NPs gel. Next, we investigated the therapeutic effect of REB nanocrystals on oral mucositis using a hamster model. Almost all of the REB was released as drug nanocrystals from the R-NPs gel, and the REB content in the cheek pouch of hamsters treated with R-NPs gel was significantly higher than that of hamsters treated with R-MPs gel. Further, treatment with REB hydrogels enhanced the healing of oral wounds in the hamsters. REB accumulation in the cheek pouch of hamsters treated with the R-NPs gel was prevented by an inhibitor of clathrin-dependent endocytosis (CME) (40 μM dynasore). In conclusion, we designed an R-NPs gel and found that REB nanocrystals are taken up by tissues through CME, where they provide a persistent effect resulting in an enhancement of oral wound healing.
Keywords: rebamipide; nanocrystals; oral mucositis; hydrogel; endocytosis rebamipide; nanocrystals; oral mucositis; hydrogel; endocytosis
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MDPI and ACS Style

Nagai, N.; Seiriki, R.; Deguchi, S.; Otake, H.; Hiramatsu, N.; Sasaki, H.; Yamamoto, N. Hydrogel Formulations Incorporating Drug Nanocrystals Enhance the Therapeutic Effect of Rebamipide in a Hamster Model for Oral Mucositis. Pharmaceutics 2020, 12, 532. https://doi.org/10.3390/pharmaceutics12060532

AMA Style

Nagai N, Seiriki R, Deguchi S, Otake H, Hiramatsu N, Sasaki H, Yamamoto N. Hydrogel Formulations Incorporating Drug Nanocrystals Enhance the Therapeutic Effect of Rebamipide in a Hamster Model for Oral Mucositis. Pharmaceutics. 2020; 12(6):532. https://doi.org/10.3390/pharmaceutics12060532

Chicago/Turabian Style

Nagai, Noriaki, Ryotaro Seiriki, Saori Deguchi, Hiroko Otake, Noriko Hiramatsu, Hiroshi Sasaki, and Naoki Yamamoto. 2020. "Hydrogel Formulations Incorporating Drug Nanocrystals Enhance the Therapeutic Effect of Rebamipide in a Hamster Model for Oral Mucositis" Pharmaceutics 12, no. 6: 532. https://doi.org/10.3390/pharmaceutics12060532

APA Style

Nagai, N., Seiriki, R., Deguchi, S., Otake, H., Hiramatsu, N., Sasaki, H., & Yamamoto, N. (2020). Hydrogel Formulations Incorporating Drug Nanocrystals Enhance the Therapeutic Effect of Rebamipide in a Hamster Model for Oral Mucositis. Pharmaceutics, 12(6), 532. https://doi.org/10.3390/pharmaceutics12060532

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