Formulation development of mucoadhesive microparticle-laden gels for oral mucositis: An in vitro and in vivo study

Hiroomi Sakurai, Yuri Ikeuchi-Takahashi, Ayaka Kobayashi, Nobuyoshi Yoshimura, Chizuko Ishihara, Tohru Aomori, Hiraku Onishi

Research output: Contribution to journalArticle

Abstract

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.

Original languageEnglish
Article number603
Pages (from-to)1-16
Number of pages16
JournalPharmaceutics
Volume12
Issue number7
DOIs
Publication statusPublished - 2020 Jul

Keywords

  • Crystal polymorph
  • Indomethacin
  • Mucoadhesive microparticles
  • Oral mucositis
  • Polyvinyl alcohol

ASJC Scopus subject areas

  • Pharmaceutical Science

Fingerprint Dive into the research topics of 'Formulation development of mucoadhesive microparticle-laden gels for oral mucositis: An in vitro and in vivo study'. Together they form a unique fingerprint.

  • Cite this

    Sakurai, H., Ikeuchi-Takahashi, Y., Kobayashi, A., Yoshimura, N., Ishihara, C., Aomori, T., & Onishi, H. (2020). Formulation development of mucoadhesive microparticle-laden gels for oral mucositis: An in vitro and in vivo study. Pharmaceutics, 12(7), 1-16. [603]. https://doi.org/10.3390/pharmaceutics12070603