Efficient oral insulin delivery enabled by transferrin-coated acid-resistant metal-organic framework nanoparticles.
basic_science · Level V
Where this comes from
- Record sourced from PubMed, PMID 35196087.
- Also identified by DOI 10.1126/sciadv.abm4677 and PMC identifier 8865763.
- Licence recorded as CC BY-NC.
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Abstract
Oral protein delivery is considered a cutting-edge technology to improve patients' quality of life, offering superior patient compliance and convenience compared with injections. However, oral protein formulation has stagnated because of the instability and inefficient penetration of protein in the gastrointestinal tract. Here, we used acid-resistant metal-organic framework nanoparticles (UiO-68-NH<sub>2</sub>) to encapsulate sufficient insulin and decorated the exterior with targeting proteins (transferrin) to realize highly efficient oral insulin delivery. The UiO-68-NH<sub>2</sub> nanocarrier with proper pore size achieved high insulin loading while protecting insulin from acid and enzymatic degradation. Through receptor-mediated transcellular pathway, the transferrin-coated nanoparticles realized efficient transport across the intestinal epithelium and controlled insulin release under physiological conditions, leading to a notable hypoglycemic effect and a high oral bioavailability of 29.6%. Our work demonstrates that functional metal-organic framework nanoparticles can protect proteins from the gastric environment and overcome the intestinal barrier, thus providing the possibility for oral biomacromolecule delivery.