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In situ pepsin-assisted needle assembly of magnetic-graphitic-nanocapsules for enhanced gastric retention and mucus penetration
Cai,Xinqi1; Xu,Yiting1; Zhao,Lina2,3; Xu,Jiamei1; Li,Shengkai1; Wen,Chaoqi1; Xia,Xin1; Dong,Qian1; Hu,Xiaoxiao1; Wang,Xiaofeng2,3; Chen,Long4; Chen,Zhuo1; Tan,Weihong1,5
2021-02-01
Source PublicationNano Today
ISSN1748-0132
Volume36
AbstractGastric environment is an extreme pH and enzyme-rich condition, which together with gastric mucus barrier and short retention time of oral medicine militate against effective oral drug delivery to lesion areas of gastric diseases. Assembly, especially shape-control assembly of magnetic nanoparticles potentially helps the site-selective drug molecule delivery. However, the harsh gastric condition, and cumbersome and strict requirements make the in situ reversible assembly remain challenging. Herein, synergistically pepsin-bridged and magnetic field-mediated morphological control of magnetic-graphitic-nanocapsules (MGNs) needle assembly (MNA) is developed in stomach for prolonged gastric retention and enhanced mucus penetration. The MNAs with good biocompatibility, large magnetic moments and unique needle-shape are formed with the help of pepsin, demonstrating superior magnetic-driven capability to overcome gastric mucus barrier. Molecular dynamics simulations reveal binding modes between MGN and amino acid residues on either side of the pepsin, indicating pepsin acts as “bridge” allowing sufficient contact among MGNs and further facilitates the needle assembly. Moreover, anticancer drug doxorubicin (DOX)-loaded MNAs demonstrate superior targeted cancer cell killing ability and boosted DOX penetration in a mouse model, which promises good bioavailability of drug molecules. The versatile MNA-based platform offers a robust strategy for effective oral drug delivery and site-selective therapy of gastric diseases.
KeywordGastric retention Harsh gastric environment Magnetic-graphitic-nanocapsule needle Mucus penetration Pepsin-assisted assembly
DOI10.1016/j.nantod.2020.101032
URLView the original
Language英语
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Cited Times [WOS]:1   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Corresponding AuthorChen,Zhuo
Affiliation1.Molecular Science and Biomedicine Laboratory,State Key Laboratory of Chemo/Biosensing and Chemometrics,College of Chemistry and Chemical Engineering,College of Life Sciences,Aptamer Engineering Center of Hunan Province,Hunan University,Changsha,410082,China
2.CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety,Institute of High Energy Physics,Chinese Academy of Sciences,Beijing,100049,China
3.University of Chinese Academy of Sciences,Beijing,101408,China
4.Faculty of Science and Technology,University of Macau,Avenida da Universidade,Taipa,999078,Macao
5.Institute of Cancer and Basic Medicine (IBMC),Chinese Academy of Sciences,The Cancer Hospital of the University of Chinese Academy of Sciences,Hangzhou,310022,China
Recommended Citation
GB/T 7714
Cai,Xinqi,Xu,Yiting,Zhao,Lina,et al. In situ pepsin-assisted needle assembly of magnetic-graphitic-nanocapsules for enhanced gastric retention and mucus penetration[J]. Nano Today,2021,36.
APA Cai,Xinqi,Xu,Yiting,Zhao,Lina,Xu,Jiamei,Li,Shengkai,Wen,Chaoqi,Xia,Xin,Dong,Qian,Hu,Xiaoxiao,Wang,Xiaofeng,Chen,Long,Chen,Zhuo,&Tan,Weihong.(2021).In situ pepsin-assisted needle assembly of magnetic-graphitic-nanocapsules for enhanced gastric retention and mucus penetration.Nano Today,36.
MLA Cai,Xinqi,et al."In situ pepsin-assisted needle assembly of magnetic-graphitic-nanocapsules for enhanced gastric retention and mucus penetration".Nano Today 36(2021).
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