# Development of oral pH-sensitive redox nanotherapeutics for gastric ulcer therapy

https://mdr.nims.go.jp/datasets/45d0842a-3d38-4fbb-86f4-70433da0cf3e

## File

- [manuscript final for submission.docx](https://mdr.nims.go.jp/filesets/e46ef392-8dbf-4d80-809e-31b4fbd794da/download) ([Detail](https://mdr.nims.go.jp/filesets/e46ef392-8dbf-4d80-809e-31b4fbd794da.md))

## Id

45d0842a-3d38-4fbb-86f4-70433da0cf3e

## Local identifier



## Visibility

open_to_public

## State

published

## Created at

2024-11-24T05:18:56.510270Z

## Updated at

2025-10-01T23:30:21.641579Z

## Published at

2025-10-01T23:18:52.264228Z

## Doi

https://doi.org/10.48505/nims.5071

## First published url

https://doi.org/10.1016/j.jconrel.2024.09.039

## Date published

2024-10-01

## Recorded date published

2024-11

## Resource type

journal_article

## Manuscript type

accepted_manuscript

## Collection



## Title

- title: Development of oral pH-sensitive redox nanotherapeutics for gastric ulcer
    therapy
  title_type: original
  lang: en

## Description

- description: Gastric ulcer is a common gastrointestinal disorder worldwide. Although
    its pathogenesis is unclear, the overproduction of reactive oxygen species (ROS),
    which results in an oxidative imbalance, has been reported as a central driving
    mechanism. Within the scope of this investigation, we developed two different
    self-assembling redox nanoparticles (RNPs) with ROS-scavenging features for the
    oral treatment of gastric ulcers. One of them, referred to as RNPN, disintegrates
    in response to acidic pH, whereas the other, denoted as RNPO, remains intact regardless
    of pH variations. Both types of RNPs showed different free radical scavenging
    activities in vitro. Protonation of the amino linkages in the side chains of RNPN
    caused the micelle structure to collapse and the nitroxide radicals encapsulated
    in the core were exposed to the outside, resulting in a significant increase in
    antioxidant capacity as the pH decreases. In contrast, RNPO maintained its spherical
    structure and consistent antioxidant reactivity irrespective of pH changes. The
    in vivo gastric retention of orally administered RNPN was significantly improved
    compared to that of RNPO which might be explained by the increased exposure of
    cationic protonating segments in RNPN on the negatively charged gastric mucosal
    surface. Owing to its improved gastric retention and enhanced ROS scavenging capacity
    under acidic pH conditions, RNPN exhibited superior protective effects against
    oxidative stress induced by aspirin in a gastric ulcer mouse model compared to
    RNPO. In addition, neither RNPN nor RNPO resulted in severe lethal effects or
    significant changes in the morphology of zebrafish embryos, indicating their biosafety.
    Our results suggest that the oral administration of RNPs has a high therapeutic
    potential for gastric ulcer treatment.
  description_type: abstract
  lang: und

## Creator

- name: Minh-Dat Quoc Tang
  role: author
- name: Nhi Bao Tran
  role: author
- name: Thu-Ha Thi Nguyen
  role: author
- name: Khanh-Uyen Hoang Nguyen
  role: author
- name: Nhu-Thuy Trinh
  role: author
- name: Toi Van Vo
  role: author
- name: Makoto Kobayashi
  role: author
- name: Toru Yoshitomi
  role: author
  orcid: https://orcid.org/0000-0003-3847-1812
  organization: National Institute for Materials Science
  ror: https://ror.org/026v1ze26
- name: Yukio Nagasaki
  role: author
- name: Long Binh Vong
  role: author

## Contact agent



## Publisher

organization: Elsevier BV

## Managing organization



## Keyword

- subject: Gastric ulcer
  schema: not_defined
- subject: pH-sensitive
  schema: not_defined
- subject: Oral delivery
  schema: not_defined
- subject: Aspirin
  schema: not_defined
- subject: ROS
  schema: not_defined
- subject: Redox nanoparticles
  schema: not_defined

## Rights

- description: "© 2024. This manuscript version is made available under the CC-BY-NC-ND
    4.0 license https://creativecommons.org/licenses/by-nc-nd/4.0/"
  identifier: https://creativecommons.org/licenses/by-nc-nd/4.0/

## Other identifier(s)



## Data origin

- data_origin_type: other

## Embargo

start_date: 2024-10-02
end_date: 2025-10-02

## Journal

- title: Journal of Controlled Release
  issn: '01683659'
  volume: '375'
  start_page: 758
  end_page: 766

## Conference



## Related item



## Funding

- funder_name: Foundation for Promotion of Material Science and Technology of Japan

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## Fileset

- id: e46ef392-8dbf-4d80-809e-31b4fbd794da
  filename: manuscript final for submission.docx
  content_type: application/vnd.openxmlformats-officedocument.wordprocessingml.document
  size: 1909109
  md5: 5bd02ae4e72bc10e5be8376c766e178e

## Thumbnail

fileset_id: e46ef392-8dbf-4d80-809e-31b4fbd794da
filename: manuscript final for submission.docx