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Open AccessArticle

Formulation Development of Mucoadhesive Microparticle-Laden Gels for Oral Mucositis: An In Vitro and In Vivo Study

1
Department of Pharmacy, Keio University Hospital, 35 Shinanomachi, Shinjuku, Tokyo 160-8582, Japan
2
Department of Drug Delivery Research, Hoshi University, 2-4-41 Ebara, Shinagawa, Tokyo 142-8501, Japan
3
Osaka R&D Center, Mitsubishi Chemical Corporation, 2-13-1 Muroyama, Ibaraki, Osaka 567-0052, Japan
4
Hospital Pharmacy Science, Keio University Faculty of Pharmacy, 1-5-30 Shibakoen, Minato, Tokyo 105-8512, Japan
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(7), 603; https://doi.org/10.3390/pharmaceutics12070603
Received: 24 April 2020 / Revised: 28 May 2020 / Accepted: 10 June 2020 / Published: 29 June 2020
(This article belongs to the Special Issue Coating Design: From Nanoparticle to Solid Dosage)
In order to relieve pain due to oral mucositis, we attempted to develop mucoadhesive microparticles containing indomethacin (IM) and gel preparations with IM microparticles that can be applied to the oral cavity. The mucoadhesive microparticles were prepared with a simple composition consisting of IM and polyvinyl alcohol (PVA). Two kinds of PVA with different block properties were used, and microparticles were prepared by heating-filtration and mixing-drying. From the X-ray powder diffraction patterns, differential scanning calorimetry thermograms, and morphological features of the IM microparticles, IM should exist as polymorphic forms in the microparticles. Rapid drug release properties were observed in the IM microparticles. Increased drug retention was observed in IM microparticles containing PVA, and the IM-NK(50) gel, using a common block character PVA and heating-filtration, showed good long-term drug retention properties. In vivo experiments showing significantly higher drug concentrations in the oral mucosa were observed with IM microparticles prepared by heating-filtration, and the IM-NK(50) gel maintained significantly higher drug concentrations in the oral mucosa. From these results, the IM-NK(50) gel may be useful as a preparation for relieving oral mucositis pain. View Full-Text
Keywords: mucoadhesive microparticles; polyvinyl alcohol; indomethacin; oral mucositis; crystal polymorph mucoadhesive microparticles; polyvinyl alcohol; indomethacin; oral mucositis; crystal polymorph
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MDPI and ACS Style

Sakurai, H.; Ikeuchi-Takahashi, Y.; Kobayashi, A.; Yoshimura, N.; Ishihara, C.; Aomori, T.; Onishi, H. Formulation Development of Mucoadhesive Microparticle-Laden Gels for Oral Mucositis: An In Vitro and In Vivo Study. Pharmaceutics 2020, 12, 603. https://doi.org/10.3390/pharmaceutics12070603

AMA Style

Sakurai H, Ikeuchi-Takahashi Y, Kobayashi A, Yoshimura N, Ishihara C, Aomori T, Onishi H. Formulation Development of Mucoadhesive Microparticle-Laden Gels for Oral Mucositis: An In Vitro and In Vivo Study. Pharmaceutics. 2020; 12(7):603. https://doi.org/10.3390/pharmaceutics12070603

Chicago/Turabian Style

Sakurai, Hiroomi; Ikeuchi-Takahashi, Yuri; Kobayashi, Ayaka; Yoshimura, Nobuyoshi; Ishihara, Chizuko; Aomori, Tohru; Onishi, Hiraku. 2020. "Formulation Development of Mucoadhesive Microparticle-Laden Gels for Oral Mucositis: An In Vitro and In Vivo Study" Pharmaceutics 12, no. 7: 603. https://doi.org/10.3390/pharmaceutics12070603

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