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Palmitic acid‐ and cysteine‐functionalized nanoparticles overcome mucus and epithelial barrier for oral delivery of drug
Nanoparticles (NPs) used for oral administration have greatly improved drug bioavailability and therapeutic efficacy. Nevertheless, NPs are limited by biological barriers, such as gastrointestinal degradation, mucus barrier, and epithelial barrier. To solve these problems, we developed the PA‐N‐2‐HA...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
John Wiley & Sons, Inc.
2023
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10189451/ https://www.ncbi.nlm.nih.gov/pubmed/37206211 http://dx.doi.org/10.1002/btm2.10510 |
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author | Xie, Yinzhuo Jin, Zheng Ma, Da Yin, Tan Hui Zhao, Kai |
author_facet | Xie, Yinzhuo Jin, Zheng Ma, Da Yin, Tan Hui Zhao, Kai |
author_sort | Xie, Yinzhuo |
collection | PubMed |
description | Nanoparticles (NPs) used for oral administration have greatly improved drug bioavailability and therapeutic efficacy. Nevertheless, NPs are limited by biological barriers, such as gastrointestinal degradation, mucus barrier, and epithelial barrier. To solve these problems, we developed the PA‐N‐2‐HACC‐Cys NPs loaded with anti‐inflammatory hydrophobic drug curcumin (CUR) (CUR@PA‐N‐2‐HACC‐Cys NPs) by self‐assembled amphiphilic polymer, composed of the N‐2‐Hydroxypropyl trimethyl ammonium chloride chitosan (N‐2‐HACC), hydrophobic palmitic acid (PA), and cysteine (Cys). After oral administration, the CUR@PA‐N‐2‐HACC‐Cys NPs had good stability and sustained release under gastrointestinal conditions, followed by adhering to the intestine to achieve drug mucosal delivery. Additionally, the NPs could penetrate mucus and epithelial barriers to promote cellular uptake. The CUR@PA‐N‐2‐HACC‐Cys NPs could open tight junctions between cells for transepithelial transport while striking a balance between mucus interaction and diffusion through mucus. Notably, the CUR@PA‐N‐2‐HACC‐Cys NPs improved the oral bioavailability of CUR, which remarkably relieved colitis symptoms and promoted mucosal epithelial repair. Our findings proved that the CUR@PA‐N‐2‐HACC‐Cys NPs had excellent biocompatibility, could overcome mucus and epithelial barriers, and had significant application prospects for oral delivery of the hydrophobic drugs. |
format | Online Article Text |
id | pubmed-10189451 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | John Wiley & Sons, Inc. |
record_format | MEDLINE/PubMed |
spelling | pubmed-101894512023-05-18 Palmitic acid‐ and cysteine‐functionalized nanoparticles overcome mucus and epithelial barrier for oral delivery of drug Xie, Yinzhuo Jin, Zheng Ma, Da Yin, Tan Hui Zhao, Kai Bioeng Transl Med Research Articles Nanoparticles (NPs) used for oral administration have greatly improved drug bioavailability and therapeutic efficacy. Nevertheless, NPs are limited by biological barriers, such as gastrointestinal degradation, mucus barrier, and epithelial barrier. To solve these problems, we developed the PA‐N‐2‐HACC‐Cys NPs loaded with anti‐inflammatory hydrophobic drug curcumin (CUR) (CUR@PA‐N‐2‐HACC‐Cys NPs) by self‐assembled amphiphilic polymer, composed of the N‐2‐Hydroxypropyl trimethyl ammonium chloride chitosan (N‐2‐HACC), hydrophobic palmitic acid (PA), and cysteine (Cys). After oral administration, the CUR@PA‐N‐2‐HACC‐Cys NPs had good stability and sustained release under gastrointestinal conditions, followed by adhering to the intestine to achieve drug mucosal delivery. Additionally, the NPs could penetrate mucus and epithelial barriers to promote cellular uptake. The CUR@PA‐N‐2‐HACC‐Cys NPs could open tight junctions between cells for transepithelial transport while striking a balance between mucus interaction and diffusion through mucus. Notably, the CUR@PA‐N‐2‐HACC‐Cys NPs improved the oral bioavailability of CUR, which remarkably relieved colitis symptoms and promoted mucosal epithelial repair. Our findings proved that the CUR@PA‐N‐2‐HACC‐Cys NPs had excellent biocompatibility, could overcome mucus and epithelial barriers, and had significant application prospects for oral delivery of the hydrophobic drugs. John Wiley & Sons, Inc. 2023-03-23 /pmc/articles/PMC10189451/ /pubmed/37206211 http://dx.doi.org/10.1002/btm2.10510 Text en © 2023 The Authors. Bioengineering & Translational Medicine published by Wiley Periodicals LLC on behalf of American Institute of Chemical Engineers. https://creativecommons.org/licenses/by/4.0/This is an open access article under the terms of the http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Articles Xie, Yinzhuo Jin, Zheng Ma, Da Yin, Tan Hui Zhao, Kai Palmitic acid‐ and cysteine‐functionalized nanoparticles overcome mucus and epithelial barrier for oral delivery of drug |
title | Palmitic acid‐ and cysteine‐functionalized nanoparticles overcome mucus and epithelial barrier for oral delivery of drug |
title_full | Palmitic acid‐ and cysteine‐functionalized nanoparticles overcome mucus and epithelial barrier for oral delivery of drug |
title_fullStr | Palmitic acid‐ and cysteine‐functionalized nanoparticles overcome mucus and epithelial barrier for oral delivery of drug |
title_full_unstemmed | Palmitic acid‐ and cysteine‐functionalized nanoparticles overcome mucus and epithelial barrier for oral delivery of drug |
title_short | Palmitic acid‐ and cysteine‐functionalized nanoparticles overcome mucus and epithelial barrier for oral delivery of drug |
title_sort | palmitic acid‐ and cysteine‐functionalized nanoparticles overcome mucus and epithelial barrier for oral delivery of drug |
topic | Research Articles |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10189451/ https://www.ncbi.nlm.nih.gov/pubmed/37206211 http://dx.doi.org/10.1002/btm2.10510 |
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