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olsalazine
SEPARATION AND PURIFICATION TECHNOLOGY · 2024 · IF 8.1

Enhancing bimetallic redox cycling by Olsalazine-based MOF to achieve efficient removal of ofloxacin

Jiayu Lu,Alu Ouyang,Zixin Wang,Yu Li,Xin Qin,Bo Su,Xuejing Huang,Kefeng Li,Jun Luo,Guorong Xu,Ling Fan,Ronghua Jin

The broad utilization of metal–organic frameworks (MOFs) in advanced oxidation processes (AOPs) for wastewater remediation is impeded by toxic ligands, the challenging recovery of catalysts, and the low cycling efficiency of metal redox pairs. In this study, we fabricated a highly efficient and self-degradable bimetallic catalyst with coordinatively unsaturated metal sites (CUMSs) using non-toxic Olsalazine (Olsa) as a ligand to effectively eliminate the antibiotic ofloxacin (OFL). Under optimal conditions, the OFL removal efficiency approached nearly 100 % within 100 min, with the degradation rate of bimetallic MOFs being 4 times than that of monometallic MOFs. The significant enhancement in catalytic performance of the catalyst was ascribed to its reduced charge transfer resistance (Rct), coordinatively unsaturated metal sites, and accelerated cycling of high valence metal to low valence metal, facilitated by the introduction of bimetallic and reducing non-toxic ligands. Moreover, we investigated the effects of H 2 O 2 concentration, catalytic dose, and pH on pollutant degradation. Additionally, results from quenching experiments and electron spin resonance (ESR) tests demonstrated that the three types of free radicals generated during the catalyst activation process played a key role in pollutant degradation.

CAS / MDL: 7758-98-7
研究领域: 环境科学 · 材料科学 · 化学工程
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Materials Today Bio · 2025 · IF 10.2

Oral olsalazine/ellagic acid/ZnCl2‐modified in situ-forming hydrogels alleviates anxiety/depression-like symptoms and brain neural activity in colitis mice

Tingting Li,Nianlu Li,Haoyu Sheng,Luyao Zhang,Qian Luo,Sashuang Liu,Yijing Zhao,Wenqiang Chen,Dexiang Liu,Zhen Wang

Inflammatory bowel disease (IBD) is a kind of chronic non-specific intestinal inflammatory disease, which accompanied by various abnormal psychological states, such as anxiety and depression. Nevertheless, the pathogenesis of IBD with depression is still unclear. Herein, we synthesized an enable a drinkable, liquid in situ-forming hydrogel, which form directly in the stomach through sequential ingestion of a crosslinker solution of CaCl 2 and ε-poly-l-lysine (ε-PL), followed by a drug-containing polymer solution of sodium alginate (SA). Using olsalazine (Olsa) and antioxidant (ellagic acid (EA) and ZnCl 2 ) as small molecule drug (referred as Olsa/EA/Zn), the resulting hydrogel (referred as Olsa/EA/Zn@SA/ε-PL hydrogel) could form rapidly in gastric fluid and exhibit remarkable stability under acidic conditions, unique low swelling properties and a rational release of drug in entering the intestine. We demonstrated that the oral administration of drug-loaded in situ-forming hydrogel with excellent antioxidant, anti-inflammatory activities, cytocompatibility, intestinal retention capacity of the drug, significantly enhanced the IBD therapeutic outcomes, and relieve accompanying depression-like symptoms in colitis mice. Overall, this designed in situ-forming hydrogel oral delivery system will open up new pathway in combined gastrointestinal therapy and psychological comorbidities for IBD patients, especially those with dysphagia.

CAS / MDL: 476-66-4 9005-38-3
研究领域: 药剂学 · 神经科学 · 胃肠病学
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BIO-MEDICAL MATERIALS AND ENGINEERING · 2023 · IF 1

Rapidly degradable konjac glucomannan hydrogels cross-linked with olsalazine for colonic drug release

Zhang Qiao,Fu Huili,Zhang Yunfei,Li Liang,Yan Guoping

BACKGROUND:Polysaccharide hydrogel is one of the most important materials for the colon target drug release system. However, the degradation time of polysaccharide hydrogel is much longer than the retention time in the colon. The drugs are expelled from the body before being released. OBJECTIVE:In order to match the degradation of drug carriers and their retention time in the colon, a rapidly degradable konjac glucomannan (KGM) hydrogel was designed for colon target drug release. METHODS:A crosslinker containing azo bond, olsalazine, was used to prepare the rapidly degradable KGM hydrogel. The degradation and drug release of the hydrogels with different crosslinking densities in the normal buffer and the human fecal medium were studied to evaluate the efficiency of colon drug release. RESULTS:More than 50% of the KGM hydrogel by weight was degraded and more than 60% of the 5-fluorouracil (5-Fu) was released within 48 h in 5% w/v human fecal medium. CONCLUSION:The drug was released more rapidly in a simulated colon environment than in a normal buffer. Furthermore, the drug release was controlled by the degradation of the hydrogel. The KGM hydrogel containing azo crosslinker has great potential for colon drug release.

研究领域: 药剂学 · 生物材料学
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BIOMACROMOLECULES · 2023 · IF 6.2

Orally Administrated Olsalazine-Loaded Multilayer Pectin/Chitosan/Alginate Composite Microspheres for Ulcerative Colitis Treatment

Jiaying Li,Yuji Pu,Sai Li,Bin He,Jianlin Chen

The pathogenesis of inflammatory bowel diseases (IBDs) including ulcerative colitis (UC) and Crohn’s disease is extremely cloudy. Maintaining the level of remission lesions in colitis is the default treatment attitude at present. Epithelial barrier restoration is considered as the same important strategy as colonic targeted drug delivery in UC treatment. In this paper, we developed a multilayer natural polysaccharide microsphere (pectin/chitosan/alginate) with pH and enzyme dual sensitivity to reduce the loss of medication in the upper digestive tract and preferentially adhere to exposed epithelial cells in colonic tissues by electrostatic forces for efficiently targeted UC treatment. Olsalazine as an inflammatory drug was efficiently loaded in the chitosan layer and realized a colonic pH-responsive drug release. Furthermore, the multilayer microspheres exhibited excellent capability in suppressing harmful flora and a bio-adhesion effect to extend the duration of local medicine. In the in vivo anti-colitis study, the downregulated levels of pro-inflammatory factors and the increase of tight junction protein indicated the excellent anti-inflammation effect of the olsalazine-loaded microspheres. In summary, these results showed that the multilayer natural polysaccharide microspheres could be a powerful candidate in the targeted drug delivery system for UC therapy.

研究领域: 药学 · 药物递送系统 · 炎症性肠病 · 生物医学工程
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JOURNAL OF COLLOID AND INTERFACE SCIENCE · 2025 · IF 9.7

A clinically inspired olsalazine-based metal-organic framework enables a universal nanodrugs platform for diverse disease

Jiayu Lu,Yu Li,Xin Qin,Zixin Wang,Alu Ouyang,Bo Su,Hongwei Guo,Xingye Yang,Zonglin Shen,Junyi Li,Ling Fan,Yandong Xie,Ronghua Jin

Conventional nanocarriers have three inherent limitations: therapeutic inefficacy, suboptimal drug-loading capacity, and disease-specific nanocarrier requirements necessitating frequent structural reconfiguration. To overcome these challenges, we developed a novel modular synergistic bioactive nanocarrier based on olsalazine (Olsa), utilizing a modular coordination-switching strategy to achieve cross-disease therapeutic adaptability. A spherical Olsa-based Cu/Fe metal-organic framework (MOF) was developed for colorectal cancer (CRC) therapy to encapsulate doxorubicin (DOX) and address the intrinsic hydrogen peroxide (H 2 O 2 ) deficiency in tumor microenvironments through a self-catalytic H 2 O 2 regeneration mechanism. This approach exhibited a 2.3 ± 0.1-fold enhancement in tumor-selective cytotoxicity and a 10.6 ± 2.2-fold enhancement in tumor accumulation efficiency. The synergistic combination of photothermal therapy (PTT), chemodynamic therapy (CDT), chemotherapy, and immunotherapy creates a self-reinforcing therapeutic cascade that concurrently mitigates therapy-induced inflammatory responses and enhances immunogenic cell death (ICD) through damage-associated molecular patterns (DAMP) activation. A biconical Ce-Olsa MOF oral nanotherapeutic was developed for ulcerative colitis (UC) management, serving as a dual-function nanocarrier that simultaneously scavenges pathogenic reactive oxygen species (ROS) and facilitates ROS-mediated mesalazine release. This spatiotemporally controlled release profile resulted in significant downregulation of pro-inflammatory cytokines and complete restoration of tight junction protein expression. This study pioneers a transformative nanocarrier that revolutionizes therapeutic nanocarrier design through three innovations: (i) the synergistic integration of therapeutic and nanocarrier functionalities using intrinsically bioactive molecules, (ii) universal disease adaptability for precision intervention across multiple pathological conditions through modular coordination switching, and (iii) clinically validated, Food and Drug Administration (FDA)-approved molecules with proven biocompatibility.

研究领域: 纳米医学 · 材料科学 · 肿瘤学 · 免疫学 · 药剂学 · 炎症性肠病研究
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EUROPEAN POLYMER JOURNAL · 2019 · IF 3.621

Enzyme and PH responsive 5-flurouracil (5-FU) loaded hydrogels based on olsalazine derivatives for colon-specific drug delivery

Zhengang Ma,Rui Ma,Xue Wang,Jinlai Gao,Yufeng Zheng,Zhijie Sun

Colon-specific drug delivery systems are efficient for increasing the availability of drugs at colon region and are desirable for the treatment of local diseases such as ulcerative colitis and colonic cancer. We synthesized an acryloyl chloride modified olsalazine (olsalazine-AC) as an azo crosslinker which was copolymerized with hydroxyethyl methacrylate (HEMA) and methacrylic acid (MAA), and developed two types of azo hydrogels which contained single network hydrogel and interpenetrating network hydrogel as an enzyme responsive and pH responsive controlled release carrier for colon-specific drug delivery. The structure of the azo crosslinker was characterized by FT-IR and 1 H NMR spectra and the azo hydrogels were analyzed by using ultraviolet spectrophotometer and scanning electron microscopy. The in vitro release of the 5-flurouracil (5-FU) loaded azo hydrogels was carried out in PBS (pH 7.4), PBS (pH 2.0) and rat colonic fluid (RCF). The drug release profile revealed that 5-FU loaded in azo hydrogels released faster in rat colonic fluid. The results showed that these azo hydrogels could be potential drug carrier for colon-targeted delivery.

研究领域: 药剂学 · 药物递送系统 · 高分子科学 · 生物医学工程 · 结肠癌治疗
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RSC Advances · 2018 ·Vol. 8 ·期 5 ·2561-2574 · IF 2.936

Colon-targeting mutual prodrugs of 5-aminosalicylic acid and butyrate for the treatment of ulcerative colitis

Yan Yan,Jinyao Sun,Xianting Xie,Pengchong Wang,Ying Sun,Yalin Dong,Jianfeng Xing

The aim of this study was to design and synthesize four colon-targeting mutual prodrugs of 5-aminosalicylic acid (5-ASA) and butyrate, and evaluate their therapeutic effects on ulcerative colitis. Herein, 5-ASB, 5-ASDB, Ols-DB and Ols-DBP were prepared and characterized, and their lipophilicity, solubility, in vitro and in vivo stability were investigated. Finally, the ameliorative effects of the prodrugs on experimental colitis were evaluated via a series of indicators, including the body weight and survival rates of mice, the colon index and colonic damage score, the disease activity index, the myeloperoxidase activity and levels of superoxide dismutase, malondialdehyde, glutathione and glutathione peroxidase in colonic tissues. As a result, 5-ASB was very stable but Ols-DB showed extreme instability in the environment of the gastrointestinal tract, while 5-ASDB and Ols-DBP showed desirable colon-targeting properties. The four prodrugs all had certain therapeutic effects on the experimental colitis. When orally administered to mice, 5-ASDB and Ols-DBP had significantly greater effects than the mixture of 5-ASA and sodium butyrate. Ols-DB was used as an enema and could be as effective as 5-ASDB and Ols-DBP. In addition, the therapeutic effects of the synthesized prodrugs might be associated with their anti-oxidative damage ability.

研究领域: 药理学 · 消化系统疾病
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