# Chloroquine-based polymer particles as oral non-absorbable treatment of inflammatory bowel disease

> **NIH NIH R01** · UNIVERSITY OF NEBRASKA MEDICAL CENTER · 2021 · $517,434

## Abstract

PROJECT SUMMARY
Inflammatory bowel disease (IBD) is a chronic inflammatory condition that affects a growing number of people
in the United States and for which there is no cure. IBD is characterized by diarrhea, pain, oxidative stress and
reactive oxygen species (ROS), and increased risk of colon cancer. There is a great need to develop better
treatments for IBD, especially treatments that act locally in the inflamed colon without whole-body exposure and
associated side effects. The goal of this proposal is to develop innovative anti-inflammatory beads for improved
treatment of IBD. The anti-inflammatory beads are designed to be given orally to the patients and engineered to
find and preferentially localize to the inflamed parts of the colon, where they respond to signals associated with
the colon inflammation and ROS to activate their therapeutic function. Because of their properties, the distribution
of the beads is restricted to the colon and they are not absorbed into the whole body like conventional IBD drugs,
thus minimizing undesired side effects during long-term chronic treatment. This project is based on our recent
discoveries and development of novel type of materials (PCQ) based on a widely used antimalarial drug
chloroquine. The overall objective of this proposal is to develop, and test oral non-absorbable therapeutic
particles designed to preferentially accumulate in, and safely reduce, colon inflammation in IBD. The central
hypothesis of this proposal is that reformulation of PCQ as inflammation-sensitive beads will lead to improved
accumulation in the inflamed parts of the colon and result in improved anti-inflammatory activity in IBD. The
hypothesis is based on (i) available evidence that orally given nano- and microparticles preferentially localize at
the IBD inflammation sites and (ii) our current studies, which demonstrate that PCQ alone enhances healing of
experimental IBD in mice. The use of inflammation-responsive particles to deliver therapeutically active polymer
(PCQ) represents an innovative approach to the local oral treatment of IBD. We will accomplish the overall
objectives by pursuing three specific aims. In Aim 1, we will prepare ROS-responsive particles based on
therapeutic PCQ. In Aim 2, we will validate the efficacy of the optimized PCQ particles in epithelial injury model
of IBD, infectious model of IBD, and in a chronic IBD model induced by the transfer of activated T cells. In Aim
3, we will determine the cellular and molecular modalities affected by the PCQ treatment.

## Key facts

- **NIH application ID:** 10135947
- **Project number:** 5R01DK124095-02
- **Recipient organization:** UNIVERSITY OF NEBRASKA MEDICAL CENTER
- **Principal Investigator:** David Oupicky
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $517,434
- **Award type:** 5
- **Project period:** 2020-04-01 → 2024-02-29

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10135947

## Citation

> US National Institutes of Health, RePORTER application 10135947, Chloroquine-based polymer particles as oral non-absorbable treatment of inflammatory bowel disease (5R01DK124095-02). Retrieved via AI Analytics 2026-05-22 from https://api.ai-analytics.org/grant/nih/10135947. Licensed CC0.

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