Adhesive polyelectrolyte coating through UV-triggered polymerization on PLGA particles for enhanced drug delivery to inflammatory intestinal mucosa

Abstract Administering medication precisely to the inflamed intestinal sites to treat ulcerative colitis (UC), with minimized side effects, is of urgent need. In UC, the inflammation damaged mucosa contains a large number of amino groups which are positively charged, providing new opportunities for...

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Main Authors: Jie Zhang, Yi-jing Yin, Xing-wang Wang, Wei-qi Lu, Zhao-yang Chen, Chao-hui Yu, Ke-feng Ren, Cheng-fu Xu
Format: Article
Language:English
Published: BMC 2025-01-01
Series:Journal of Nanobiotechnology
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Online Access:https://doi.org/10.1186/s12951-024-03066-3
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author Jie Zhang
Yi-jing Yin
Xing-wang Wang
Wei-qi Lu
Zhao-yang Chen
Chao-hui Yu
Ke-feng Ren
Cheng-fu Xu
author_facet Jie Zhang
Yi-jing Yin
Xing-wang Wang
Wei-qi Lu
Zhao-yang Chen
Chao-hui Yu
Ke-feng Ren
Cheng-fu Xu
author_sort Jie Zhang
collection DOAJ
description Abstract Administering medication precisely to the inflamed intestinal sites to treat ulcerative colitis (UC), with minimized side effects, is of urgent need. In UC, the inflammation damaged mucosa contains a large number of amino groups which are positively charged, providing new opportunities for drug delivery system design. Here, we report an oral drug delivery system utilizing the tacrolimus-loaded poly (lactic-co-glycolic acid) (TAC/PLGA) particles with an adhesion coating by in situ UV-triggered polymerization of polyacrylic acid and N-hydroxysuccinimide (PAA-NHS). The negatively charged carboxyl groups effectively interact with the positively charged focal mucosa, and the NHS ester groups form the covalent bonds with the amino groups, thereby synergically enhancing the adhesion of the PLGA particles to the focal mucosa. Our findings reveal that, compared to the naked particles, the PAA-NHS coating increases the adhesion of particles to the inflammatory intestine. In a dextran sulfate sodium-induced acute colitis mouse model, the TAC/PLGA particles with PAA-NHS coating exhibits substantial retention of TAC within the inflammatory intestine, enhancing drug delivery efficiency and therapeutic effects. This approach holds promise for UC management, minimizing systemic side effects and optimizing therapeutic outcomes. Graphical abstract
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institution Kabale University
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language English
publishDate 2025-01-01
publisher BMC
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series Journal of Nanobiotechnology
spelling doaj-art-c39531c0fc744e1d833d459a21ca5c042025-01-26T12:50:59ZengBMCJournal of Nanobiotechnology1477-31552025-01-0123111610.1186/s12951-024-03066-3Adhesive polyelectrolyte coating through UV-triggered polymerization on PLGA particles for enhanced drug delivery to inflammatory intestinal mucosaJie Zhang0Yi-jing Yin1Xing-wang Wang2Wei-qi Lu3Zhao-yang Chen4Chao-hui Yu5Ke-feng Ren6Cheng-fu Xu7Department of Gastroenterology, the First Affiliated Hospital, Zhejiang University School of MedicineMOE Key Laboratory of Macromolecular Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang UniversityMOE Key Laboratory of Macromolecular Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang UniversityMOE Key Laboratory of Macromolecular Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang UniversityMOE Key Laboratory of Macromolecular Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang UniversityDepartment of Gastroenterology, the First Affiliated Hospital, Zhejiang University School of MedicineMOE Key Laboratory of Macromolecular Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang UniversityDepartment of Gastroenterology, the First Affiliated Hospital, Zhejiang University School of MedicineAbstract Administering medication precisely to the inflamed intestinal sites to treat ulcerative colitis (UC), with minimized side effects, is of urgent need. In UC, the inflammation damaged mucosa contains a large number of amino groups which are positively charged, providing new opportunities for drug delivery system design. Here, we report an oral drug delivery system utilizing the tacrolimus-loaded poly (lactic-co-glycolic acid) (TAC/PLGA) particles with an adhesion coating by in situ UV-triggered polymerization of polyacrylic acid and N-hydroxysuccinimide (PAA-NHS). The negatively charged carboxyl groups effectively interact with the positively charged focal mucosa, and the NHS ester groups form the covalent bonds with the amino groups, thereby synergically enhancing the adhesion of the PLGA particles to the focal mucosa. Our findings reveal that, compared to the naked particles, the PAA-NHS coating increases the adhesion of particles to the inflammatory intestine. In a dextran sulfate sodium-induced acute colitis mouse model, the TAC/PLGA particles with PAA-NHS coating exhibits substantial retention of TAC within the inflammatory intestine, enhancing drug delivery efficiency and therapeutic effects. This approach holds promise for UC management, minimizing systemic side effects and optimizing therapeutic outcomes. Graphical abstracthttps://doi.org/10.1186/s12951-024-03066-3Ulcerative colitisAdhesive coatingUV-triggered polymerizationPLGA particlesDrug delivery
spellingShingle Jie Zhang
Yi-jing Yin
Xing-wang Wang
Wei-qi Lu
Zhao-yang Chen
Chao-hui Yu
Ke-feng Ren
Cheng-fu Xu
Adhesive polyelectrolyte coating through UV-triggered polymerization on PLGA particles for enhanced drug delivery to inflammatory intestinal mucosa
Journal of Nanobiotechnology
Ulcerative colitis
Adhesive coating
UV-triggered polymerization
PLGA particles
Drug delivery
title Adhesive polyelectrolyte coating through UV-triggered polymerization on PLGA particles for enhanced drug delivery to inflammatory intestinal mucosa
title_full Adhesive polyelectrolyte coating through UV-triggered polymerization on PLGA particles for enhanced drug delivery to inflammatory intestinal mucosa
title_fullStr Adhesive polyelectrolyte coating through UV-triggered polymerization on PLGA particles for enhanced drug delivery to inflammatory intestinal mucosa
title_full_unstemmed Adhesive polyelectrolyte coating through UV-triggered polymerization on PLGA particles for enhanced drug delivery to inflammatory intestinal mucosa
title_short Adhesive polyelectrolyte coating through UV-triggered polymerization on PLGA particles for enhanced drug delivery to inflammatory intestinal mucosa
title_sort adhesive polyelectrolyte coating through uv triggered polymerization on plga particles for enhanced drug delivery to inflammatory intestinal mucosa
topic Ulcerative colitis
Adhesive coating
UV-triggered polymerization
PLGA particles
Drug delivery
url https://doi.org/10.1186/s12951-024-03066-3
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