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<p>This study aimed to improve the oral retention of GGsTop<sup>®</sup>, a γ-glutamyl transpeptidase (GGT) inhibitor, by using a PLGA-PEG-PLGA triblock copolymer composed of polylactic-polyglycolic acid (PLGA) and polyethylene glycol (PEG) as a gel base. This copolymer is biodegradable, biocompatible, and temperature responsive. Viscoelasticity measurements revealed that the aqueous solution of the PLGA-PEG-PLGA triblock copolymer began to gel at approximately 37 °C and was maintained at approximately 43 °C. Compared with the GGsTop<sup>®</sup> aqueous solution, the incorporation of GGsTop<sup>®</sup> into the gel markedly suppressed its release from 15 min after the start of testing, demonstrating the sustained release of GGsTop<sup>®</sup>. In a mouse model of chemotherapy-induced stomatitis, compared with the GGsTop aqueous solution, the topical application of the GGsTop<sup>®</sup>-loaded gel formulation significantly reduced the lesion area and shortened the treatment period. Additionally, a significant decrease in the levels of reduced glutathione, an indicator of oxidative stress, was observed. These results suggest that the prepared gel formulation enhances the oral retention of GGsTop<sup>®</sup> and improves its therapeutic efficacy. On the basis of the above findings, the GGsTop<sup>®</sup>-loaded gel formulation was shown to be effective against stomatitis, a side effect of cancer treatment.</p>

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Development of a temperature-responsive gel formulation containing GGsTop® for treating stomatitis, a side effect of anticancer drug therapy

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年6月3日

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  • Ritsuki Okada,
  • Issei Takeuchi,
  • Shoko Itakura,
  • Kosuke Kusamori,
  • Makiya Nishikawa,
  • Akiyoshi Saitoh

摘要

This study aimed to improve the oral retention of GGsTop®, a γ-glutamyl transpeptidase (GGT) inhibitor, by using a PLGA-PEG-PLGA triblock copolymer composed of polylactic-polyglycolic acid (PLGA) and polyethylene glycol (PEG) as a gel base. This copolymer is biodegradable, biocompatible, and temperature responsive. Viscoelasticity measurements revealed that the aqueous solution of the PLGA-PEG-PLGA triblock copolymer began to gel at approximately 37 °C and was maintained at approximately 43 °C. Compared with the GGsTop® aqueous solution, the incorporation of GGsTop® into the gel markedly suppressed its release from 15 min after the start of testing, demonstrating the sustained release of GGsTop®. In a mouse model of chemotherapy-induced stomatitis, compared with the GGsTop aqueous solution, the topical application of the GGsTop®-loaded gel formulation significantly reduced the lesion area and shortened the treatment period. Additionally, a significant decrease in the levels of reduced glutathione, an indicator of oxidative stress, was observed. These results suggest that the prepared gel formulation enhances the oral retention of GGsTop® and improves its therapeutic efficacy. On the basis of the above findings, the GGsTop®-loaded gel formulation was shown to be effective against stomatitis, a side effect of cancer treatment.