Journal of Functional Foods
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2018
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IF 3.47
Yingshu Feng,Yuan Zhu,Jinyi Wan,Xia Yang,Caleb Kesse Firempong,Jiangnan Yu,Ximing Xu
The study was aimed at formulating self-assembled capsaicin prodrug nanoparticles (Cap-SSVE NPs) with improved bioavailability, increased antihyperlipidemic activity and less gastrointestinal mucosa irritations. The in vitro release profile of the developed Cap-SSVE NPs was stable in HCl solution (pH 1.2) and distilled water, but very susceptible in PBS (pH 6.8 and 7.4). The relative oral bioavailability of Cap-SSVE NPs was 3.2 folds higher than free capsaicin, with an extended T max (0.25–1 h). The Cap-SSVE NPs decreased certain lipid profile indices of both the liver tissue (Total lipids and TG) and the blood sample (TC, TG, LDL and TBA) with elevated levels of HDL in high fat diet induced hyperlipidemic rats. The nanoparticles also predominantly accumulated in the liver with reduced irritations in the gastrointestinal mucosa . Collectively, the formulated Cap-SSVE NPs showed an enhanced bioavailability, increased hypolipidemic effects and reduced mucosa irritations.
研究领域:
药剂学
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生物医学工程
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代谢研究
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产品关联
DOI
高影响因子
Drug Design Development and Therapy
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2023
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IF 4.8
Kai Dong,Shu-Jing Deng,Bin-Yang He,Zi-Yang Guo,Ze-Lin Guan,Xue Leng,Rui-Rui Ma,Dan-Yang Wang,Jian-Feng Xing,Cui-Yu You
Background As the first-line drug to treat ulcerative colitis (UC), long-term use of glucocorticoids (GCs) produces severe toxic and side effects. Local administration as enema can increase the local GCs concentrations and reduce systemic exposure to high oral doses by directly delivering GCs to the inflammation site in the distal colorectum. However, UC patients are often accompanied by diarrhea, leading to the short colonic residence time of GCs and failure to exert their function fully.Purpose A kind of mucoadhesive nanoparticles (NPs) loading different dexamethasone derivatives (DDs) were developed, which could attach to the positively charged inflammatory colonic mucosa through electrostatic adsorption after administered by enema, thereby improving the local concentration and achieving effective targeted therapy for UC.Methods Two DDs, dexamethasone hemisuccinate and dexamethasone phosphate, were synthesized. In NPs preparation, The core PEI-DDs NPs were built by the electrostatic adsorption of DDs and the cationic polymer polyethyleneimine (PEI). Then, the natural polyanionic polysaccharide sodium alginate (SA) was electronically coated around NPs to construct the final SA-PEI-DDs NPs, followed by the in vitro stability and release tests, in vitro and in vivo colonic mucosal adhesion tests. In the in vivo anti-UC test, the experimental colitis mice were induced by 2,4,6-trinitrobenzenesulfonic acid. The body weight and disease activity index changes were measured, and the myeloperoxidase activity, pro-inflammatory cytokines concentration, and hematoxylin and eosin staining were also investigated to evaluate the therapeutic effect of NPs.Results The structures of two DDs were demonstrated by 1H-NMR and MS. Both NPs were negatively charged and achieved high loading efficiency of DDs, while their particle sizes were significantly different. NPs showed good stability and sustained release properties in the simulated colonic environment. Moreover, the negative charge on the of NPs surface made them easier to adhere to the positively charged inflammatory colonic mucosa, thereby enhancing the enrichment and retention of DDS in the colitis site. Furthermore, the NPs exhibited better therapeutic effects than free Dex on the experimental colitis mice induced by TNBS through the enema rectal.Conclusion These results indicated the mucoadhesive NPs as a kind of novel nano-enema showed great potential to achieve efficient treatment on UC.
研究领域:
药剂学
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药理学
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纳米技术
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炎症性肠病
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产品关联
DOI
PubMed
高影响因子
Food Bioscience
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2023
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IF 5.2
Shuna Chen,Jiaxin Kang,Huanqing Zhu,Ziyi Han,Leyu Wang,Kaixi Wang,Junsheng Liu,Yuanyuan Wu,Puming He,Youying Tu,Bo Li
The impacts of tea seed saponins (TSS) on intestinal injury, immune disorder, gut microbial dysbiosis and serum metabolome in cyclophosphamide (CTX)-induced mice were explored. The findings indicated that TSS significantly reversed the spleen index, protected intestinal mucosa , and increased the protein levels of tumor necrosis factor-α (TNF-α), occludin , interleukin-6 (IL-6) and immunoglobulin A (IgA) in colon and small intestine of mice. Microbiome analysis suggested that TSS shaped the gut microbial community structure, and mainly increased the proportion of Bacillus and Alloprevotella . The in vitro experiment further demonstrated the ability of TSS to promote the growth of Bacillus . Serum metabolome analysis showed that TSS significantly upregulated and downregulated 18 and 15 metabolites, respectively. Eight of these compounds were correlated with Bacillus and Alloprevotella . Over all, this work demonstrated that TSS could improve CTX-induced immune imbalance, intestinal barrier disruption and gut microbial dysbiosis, and was a potential candidate for regulating intestinal homeostasis .
研究领域:
药理学
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免疫学
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微生物学
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代谢组学
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胃肠病学
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产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）