In situ pepsin-assisted needle assembly of magnetic-graphitic-nanocapsules for enhanced gastric retention and mucus penetration

doi:10.1016/j.nantod.2020.101032

	In situ pepsin-assisted needle assembly of magnetic-graphitic-nanocapsules for enhanced gastric retention and mucus penetration
	Cai, Xinqi 1; Xu, Yiting 1; Zhao, Lina 2,3; Xu, Jiamei 1; Li, Shengkai 1; Wen, Chaoqi 1; Xia, Xin 1; Dong, Qian 1; Hu, Xiaoxiao 1; Wang, Xiaofeng 2,3
刊名	NANO TODAY
	2021-02-01
卷号	36
关键词	Harsh gastric environment Pepsin-assisted assembly Magnetic-graphitic-nanocapsule needle Gastric retention Mucus penetration
ISSN号	1748-0132
DOI	10.1016/j.nantod.2020.101032
通讯作者	Chen, Zhuo(zhuochen@hnu.edu.cn)
英文摘要	Gastric 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. (C) 2020 Elsevier Ltd. All rights reserved.
资助项目	National Natural Science Foundation of China[21522501] ; National Natural Science Foundation of China[31971311] ; National Natural Science Foundation of China[21727817] ; National Natural Science Foundation of China[61527806] ; National Natural Science Foundation of China[31701249] ; National Natural Science Foundation of China[31970692] ; Hunan Provincial Natural Science Foundation of China[2018JJ1007] ; Changsha Science and Technology Plan[kq2004009] ; High level foreign expert introduction program[GX20200018001] ; Science and Technology Development Fund, Macau[196/2017/A3]
WOS研究方向	Chemistry ; Science & Technology - Other Topics ; Materials Science
语种	英语
出版者	ELSEVIER SCI LTD
WOS记录号	WOS:000637808000024
资助机构	National Natural Science Foundation of China ; Hunan Provincial Natural Science Foundation of China ; Changsha Science and Technology Plan ; High level foreign expert introduction program ; Science and Technology Development Fund, Macau
内容类型	期刊论文
源URL	[http://ir.hfcas.ac.cn:8080/handle/334002/121938]
专题	中国科学院合肥物质科学研究院
通讯作者	Chen, Zhuo
作者单位	1.Hunan Univ, Mol Sci & Biomed Lab, State Key Lab Chemo Biosensing & Chemometr, Coll Chem & Chem Engn,Coll Life Sci,Aptamer Engn, Changsha 410082, Hunan, Peoples R China 2.Chinese Acad Sci, Inst High Energy Phys, CAS Key Lab Biomed Effects Nanomat & Nanosafety, Beijing 100049, Peoples R China 3.Univ Chinese Acad Sci, Beijing 101408, Peoples R China 4.Univ Macau, Fac Sci & Technol, Ave Univ, Taipa 999078, Macau, Peoples R China 5.Univ Chinese Acad Sci, Inst Canc & Basic Med IBMC, Chinese Acad Sci, Canc Hosp, Hangzhou 310022, Zhejiang, Peoples R China
推荐引用方式 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.,...&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).