Development and Characterization of Oral Spray for Stomatitis Containing Irsogladine Maleate

Chem Pharm Bull (Tokyo). 2016 Dec 1;64(12):1659-1665. doi: 10.1248/cpb.c16-00217. Epub 2016 Sep 15.

Abstract

The stomatitis caused by anticancer agents and radiation therapy deteriorates patient QOL, potentially causing eating disorders as a result of pain. Although gargling and ointments can be used in the treatment of stomatitis, patients must spit out mouthwash after use, while ointment application requires a finger to be inserted into the oral cavity. In contrast, sprays eliminate these potential compliance problems. Therefore, we developed a stomatitis spray that remains on the oral mucosa. It has been reported that irsogladine maleate (IM) is effective against stomatitis via oral administration. IM is water insoluble; thus, it was dissolved with various cyclodextrins (CDs). Furthermore, we examined combination with gum ghatti (GG), a mucoadhesive polymer. The interaction between mucin and GG was examined by Quartz Crystal Microbalance with Dissipation monitoring. We found that GG exhibited mucoadhesion. Furthermore, we examined the healing effects of IM on stomatitis in a stomatitis model hamster. We found that stomatitis healed after direct application of IM. However, the model used in this experiment is not based on stomatitis caused by anticancer agents. Further study is therefore necessary.

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / adverse effects
  • Antineoplastic Agents / therapeutic use
  • Disease Models, Animal
  • Male
  • Mesocricetus
  • Oral Sprays*
  • Stomatitis / chemically induced
  • Stomatitis / drug therapy*
  • Triazines / administration & dosage*
  • Triazines / therapeutic use*

Substances

  • Antineoplastic Agents
  • Oral Sprays
  • Triazines
  • irsogladine