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A PepT1 mediated medicinal nano-system for targeted delivery of cyclosporine A to alleviate acute severe ulcerative colitis

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Abstract

To effectively alleviate acute severe ulcerative colitis (ASUC), we developed a colon-specific delivery system—PLGA–KPV/MMT/CS multifunctional medicinal nanoparticles loaded with cyclosporine A (CyA). The lysine–proline–valine (KPV) tripeptide, which possesses anti-inflammatory properties and high affinity to peptide transporter 1 (PepT1), can target therapy-related cells (colonic epithelial cells and macrophages) via overexpression of PepT1. Montmorillonite (MMT)/chitosan (CS) coating can reduce CyA leakage in the upper gastrointestinal tract (GIT) and enhance nanoparticle adhesion to the inflamed colon. The bio-distribution demonstrated that nanoparticles can specifically accumulate in the inflamed tissues and can be retained for up to 36 h. After being treated with the CyA–PLGA–KPV/MMT/CS nanoparticles (PKMCN), the mice with DSS-induced ulcerative colitis exhibited significant improvements in body weight, colon length, and disease activity index. Moreover, biochemistry and immunohistochemical analysis showed that the PKMCN treatment group performed as well as the healthy group. Intriguingly, PKMCN without CyA also presented marked therapeutic effects. Our results suggested that PKMCN could be a promising drug delivery system for ASUC therapy by targeting inflamed cells, prolonging curative time, and mitigating colitis.

Graphical abstract: A PepT1 mediated medicinal nano-system for targeted delivery of cyclosporine A to alleviate acute severe ulcerative colitis

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Publication details

The article was received on 14 Jun 2019, accepted on 26 Jul 2019 and first published on 29 Jul 2019


Article type: Paper
DOI: 10.1039/C9BM00925F
Biomater. Sci., 2019, Advance Article

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    A PepT1 mediated medicinal nano-system for targeted delivery of cyclosporine A to alleviate acute severe ulcerative colitis

    Y. Wu, M. Sun, D. Wang, G. Li, J. Huang, S. Tan, L. Bao, Q. Li, G. Li and L. Si, Biomater. Sci., 2019, Advance Article , DOI: 10.1039/C9BM00925F

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