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Lentinan-Based Oral Nanoparticle Loaded Budesonide With Macrophage-Targeting Ability for Treatment of Ulcerative Colitis
Lin, Meisi1,2,3; Dong, Lingling1; Chen, Qiyan1; Xu, Haiting1; Han, Xiaoqin1; Luo, Ruifeng1; Pu, Xiulan1; Qi, Shanshan1; Nie, Wenbiao1; Ma, Meilin1; Wang, Yitao1,4; Gao, Fei1; Zhang, Jinming1
2021-08-27
Source PublicationFrontiers in Bioengineering and Biotechnology
ISSN2296-4185
Volume9
Abstract

Ulcerative colitis (UC) is a global, chronic, and refractory disease. Corticosteroids are first-line drugs for the treatment of UC but also cause adverse side effects. Budesonide (BUD), a corticosteroid with relatively low side effects, has been approved by the Food and Drug Administration for use as enteric capsules (Entocort EC) for the treatment of inflammatory bowel disease (IBD). However, this formulation lacks specific targeting ability to UC lesions. Herein, we describe the development of an advanced macrophage-targeted oral lentinan (LNT)–based nanoparticles (NPs) loaded BUD for treatment of UC. Briefly, LNT was used as a food source and natural carrier to load BUD by a simple solvent evaporation method to form LNT/BUD-NPs. LNT showed good loading capacity with high encapsulation and loading efficiencies to BUD of approximately 92.19 and 9.58%, respectively. Evaluation of the gastric stability of LNT/BUD-NPs indicated that LNT could effectively protect BUD from gastric acid and digestive enzymes. The release behavior and transmission electron microscopy image of LNT/BUD-NPs in the intestinal content of mice confirmed that intestinal flora can promote BUD release from LNT. Moreover, evaluation of cellular uptake showed that LNT/BUD-NPs could specifically target macrophages and enhance their uptake rate via the Dectin-1 receptor. In biodistribution studies, LNT/BUD-NPs were able to efficiently accumulate in the inflamed colon of mice. As expected, LNT/BUD-NPs could significantly alleviate inflammation by inhibiting the TLR4/MyD88/NF-κB signaling pathway. Therefore, LNT/BUD-NPs have the advantages of good gastric stability, release mediated by mouse intestinal content, macrophage-targeting, and anti-UC effects. These advantages indicate LNT-based NPs are a promising oral drug delivery system for UC therapy.

KeywordBudesonide Lentinan Macrophage-target Oral Nanoparticles Ulcerative Colitis
DOI10.3389/fbioe.2021.702173
URLView the original
Indexed BySCIE
Language英語English
WOS Research AreaBiotechnology & Applied Microbiology ; Science & Technology - Other Topics
WOS SubjectBiotechnology & Applied Microbiology ; Multidisciplinary Sciences
WOS IDWOS:000722698100001
Scopus ID2-s2.0-85114735267
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Cited Times [WOS]:3   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Corresponding AuthorGao, Fei; Zhang, Jinming
Affiliation1.State Key Laboratory of Southwestern Chinese Medicine Resources, Pharmacy School, Chengdu University of Traditional Chinese Medicine, Chengdu, China
2.Affiliated Hospital, Chengdu University of Traditional Chinese Medicine, Chengdu, China
3.Sichuan Provincial Acupuncture School, Chengdu, China
4.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China
Recommended Citation
GB/T 7714
Lin, Meisi,Dong, Lingling,Chen, Qiyan,et al. Lentinan-Based Oral Nanoparticle Loaded Budesonide With Macrophage-Targeting Ability for Treatment of Ulcerative Colitis[J]. Frontiers in Bioengineering and Biotechnology,2021,9.
APA Lin, Meisi,Dong, Lingling,Chen, Qiyan,Xu, Haiting,Han, Xiaoqin,Luo, Ruifeng,Pu, Xiulan,Qi, Shanshan,Nie, Wenbiao,Ma, Meilin,Wang, Yitao,Gao, Fei,&Zhang, Jinming.(2021).Lentinan-Based Oral Nanoparticle Loaded Budesonide With Macrophage-Targeting Ability for Treatment of Ulcerative Colitis.Frontiers in Bioengineering and Biotechnology,9.
MLA Lin, Meisi,et al."Lentinan-Based Oral Nanoparticle Loaded Budesonide With Macrophage-Targeting Ability for Treatment of Ulcerative Colitis".Frontiers in Bioengineering and Biotechnology 9(2021).
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