# A Novel Oral Insulin Enabling Safe and Efficient Gastrointestinal Transport and Absorption

> **NIH NIH R01** · WAYNE STATE UNIVERSITY · 2021 · $425,111

## Abstract

Project Summary
Oral insulin will improve the life quality of diabetes patients but current oral protein formulations
face multiple obstacles during their gastrointestinal transport and absorption resulting in low
therapeutic functionality. In particular, penetrating the intestinal mucus layer and the epithelial
cell layer to reach the blood remained two major challenges for any oral formulation. Despite
advancement in mucus-penetrating and absorption-enhancing technologies, current oral
delivery of protein drugs remains low in absorption and bioavailability, and/or increases the risk
of leaky gut and safety concerns such as autoimmune disease, bacterial infection and
inflammatory bowel diseases. There is an urgent need for a safe and efficient oral delivery
technology to drastically enhance protein transport through the mucus and intestinal epithelium,
and to enable oral insulin with high bioavailability. The long-term research goal of the PI is to
develop a platform technology that addresses these barriers altogether and enables oral insulin
feasible for clinical translation. The objective of this project is to explore the mechanism for a
novel insulin delivery system in addressing the mucus transport, epithelium absorption, and gut-
related safety issues and contributing to a high oral bioavailability. Specific aims include the
identification of mechanism/key parameters of the delivery system contributing to the preferred
properties and performance in addressing these obstacles through in vitro and in vivo studies
(involving diabetic mice and rats). Furthermore, this project will validate the feasibility of the oral
insulin prototype on diabetic minipigs, which is a more relevant large animal model for predicting
oral bioavailability in humans. The success of this project will directly lead to the development of
highly promising oral insulin– a life-changing treatment for diabetes patients. This project will
also produce foundational knowledge regarding how the particular delivery platform addresses
the multiple barriers for oral protein delivery; this will impact a broad range of future
development of oral protein drugs.

## Key facts

- **NIH application ID:** 10163183
- **Project number:** 5R01DK123293-03
- **Recipient organization:** WAYNE STATE UNIVERSITY
- **Principal Investigator:** Zhiqiang Cao
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $425,111
- **Award type:** 5
- **Project period:** 2019-09-25 → 2023-05-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10163183

## Citation

> US National Institutes of Health, RePORTER application 10163183, A Novel Oral Insulin Enabling Safe and Efficient Gastrointestinal Transport and Absorption (5R01DK123293-03). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/10163183. Licensed CC0.

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