Directed self-assembly of herbal small molecules into sustained release hydrogels for treating neural inflammation

Jun Zheng, Rong Fan, Huiqiong Wu, Honghui Yao, Yujie Yan, Jiamiao Liu, Lu Ran, Zhifang Sun, Lunzhao Yi, Li Dang, Pingping Gan, Piao Zheng, Tilong Yang, Yi Zhang (), Tao Tang () and Yang Wang ()
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Jun Zheng: Central South University
Rong Fan: Central South University
Huiqiong Wu: Central South University
Honghui Yao: Central South University
Yujie Yan: Central South University
Jiamiao Liu: Central South University
Lu Ran: Kunming University of Science and Technology
Zhifang Sun: Central South University
Lunzhao Yi: Kunming University of Science and Technology
Li Dang: Shantou University
Pingping Gan: Central South University
Piao Zheng: Hunan University of Chinese Medicine
Tilong Yang: Southern University of Science and Technology
Yi Zhang: Central South University
Tao Tang: Central South University
Yang Wang: Central South University

Nature Communications, 2019, vol. 10, issue 1, 1-12

Abstract: Abstract Self-assembling natural drug hydrogels formed without structural modification and able to act as carriers are of interest for biomedical applications. A lack of knowledge about natural drug gels limits there current application. Here, we report on rhein, a herbal natural product, which is directly self-assembled into hydrogels through noncovalent interactions. This hydrogel shows excellent stability, sustained release and reversible stimuli-responses. The hydrogel consists of a three-dimensional nanofiber network that prevents premature degradation. Moreover, it easily enters cells and binds to toll-like receptor 4. This enables rhein hydrogels to significantly dephosphorylate IκBα, inhibiting the nuclear translocation of p65 at the NFκB signalling pathway in lipopolysaccharide-induced BV2 microglia. Subsequently, rhein hydrogels alleviate neuroinflammation with a long-lasting effect and little cytotoxicity compared to the equivalent free-drug in vitro. This study highlights a direct self-assembly hydrogel from natural small molecule as a promising neuroinflammatory therapy.

Date: 2019
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DOI: 10.1038/s41467-019-09601-3

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