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Oral Colon-Targeted Konjac Glucomannan Hydrogel Constructed through Noncovalent Cross-Linking by Cucurbit[8]uril for Ulcerative Colitis Therapy
Ding,Yuan Fu1; Sun,Tianlei1; Li,Shengke1; Huang,Qiaoxian1; Yue,Ludan1; Zhu,Liangkui2; Wang,Ruibing1
2020-01-21
Source PublicationACS Applied Bio Materials
Volume3Issue:1Pages:10-19
AbstractOrally administered colon-targeted formulations of drugs are of great importance in managing diseases in the colon. However, it is often challenging to maintain the integrity of such formulations during delivery, particularly in the gastric environment, which may lead to premature drug release before reaching the targeted colon. Herein, an oral colon-targeted drug delivery hydrogel (OCDDH) was developed through cucurbit[8]uril (CB[8])-mediated noncovalent cross-linking of phenylalanine (Phe)-modified Konjac glucomannan (KGM), in which berberine (BBR), a natural anti-inflammatory product originating from Chinese medicine, was loaded into the hydrogel matrix. With the strong host-guest complexation mediated cross-linking and the inherent reversibility of such interactions, KGM-Phe@CB[8] hydrogel exhibited a readily tunable degree of cross-linking and an excellent self-healing capability, and therefore the hydrogel retained ultrahigh stability in the gastric environment, which is important for orally administered formulations to target the colon. In the colon, KGM may get degraded by colon-specific enzymes, β-mannanase or β-glucosidase, resulting in burst release of the loaded cargoes on site. The structure and specific payload release of the hydrogel, with and without BBR, have been fully characterized in vitro, and the therapeutic effect of BBR-loaded KGM-Phe@CB[8] hydrogel was evaluated against dextran sulfate sodium (DSS) induced ulcerative colitis (UC) in a mouse model. Very interestingly, the BBR-loaded KGM-Phe@CB[8] hydrogel exhibited significantly improved therapeutic efficacy in treating colitis, without causing any systemic toxicity, when compared with free BBR. This strategy may pave a new way in the development of advanced supramolecular OCDDH.
Keywordcolitis controlled drug release cucurbituril host-guest interactions Konjac glucomannan
DOI10.1021/acsabm.9b00676
URLView the original
Language英语
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Cited Times [WOS]:7   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Corresponding AuthorWang,Ruibing
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine,Institute of Chinese Medical Sciences,University of Macau,Taipa,999078,Macao
2.State Key Laboratory of Inorganic Synthesis and Preparative Chemistry,Jilin University,Changchun,130012,China
First Author AffilicationInstitute of Chinese Medical Sciences
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Ding,Yuan Fu,Sun,Tianlei,Li,Shengke,et al. Oral Colon-Targeted Konjac Glucomannan Hydrogel Constructed through Noncovalent Cross-Linking by Cucurbit[8]uril for Ulcerative Colitis Therapy[J]. ACS Applied Bio Materials,2020,3(1):10-19.
APA Ding,Yuan Fu,Sun,Tianlei,Li,Shengke,Huang,Qiaoxian,Yue,Ludan,Zhu,Liangkui,&Wang,Ruibing.(2020).Oral Colon-Targeted Konjac Glucomannan Hydrogel Constructed through Noncovalent Cross-Linking by Cucurbit[8]uril for Ulcerative Colitis Therapy.ACS Applied Bio Materials,3(1),10-19.
MLA Ding,Yuan Fu,et al."Oral Colon-Targeted Konjac Glucomannan Hydrogel Constructed through Noncovalent Cross-Linking by Cucurbit[8]uril for Ulcerative Colitis Therapy".ACS Applied Bio Materials 3.1(2020):10-19.
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