APPLIED SURFACE SCIENCE
·
2019
·
IF 5.155
Hui Li,Yanlin Zhang,Qian Zhang,Yifei Wang,Yanping Fan,Xin Gao,Jing Niu
In our work, Z -scheme Ag 3 PO 4 /NG/WO 3 composites were fabricated via a facile deposition approach, which was used in the photocatalytic degradation of indomethacin (IDM) under visible light irradiation. The as-prepared Ag 3 PO 4 -based photocatalysts were characterized by X-ray diffraction analysis, scanning electron microscopy, transmission electron microscope , Fourier transform infrared, X-ray photoelectron spectroscopy and UV–visible diffuse reflectance spectroscopy in order to determine the chemical structure , morphological feature and optical performance. From the degradation experiments of IDM, the Ag 3 PO 4 /NG/WO 3 composite exhibited the highest photocatalytic activity and stability, and its kinetics constant was ~8 times of pure Ag 3 PO 4 . Furthermore, reactive species trapping experiment, electron spin resonance , liquid chromatography-mass spectrometry, total organic carbon , photoelectrochemical measurement and photoluminescence spectra were applied to analyze the possible degradation pathways and photocatalytic mechanism of IDM. The results indicated that the visible-light photocatalytic degradation of IDM using Ag 3 PO 4 /NG/WO 3 conformed to a Z -scheme photocatalysis mechanism, further facilitating the photoinduced charge carriers separation, and inhibiting the recombination of photoinduced electron-hole pairs. It also confirmed that the holes, OH and O 2 – radicals generated in Z -scheme system played the significant roles during the photocatalytic degradation of IDM.
研究领域:
环境科学
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材料科学
·
光化学
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DOI
高影响因子
PLoS One
·
2017
·Vol. 12
·期 7
·e0180037
·
IF 2.806
Weiping Ji,Bo Wang,Qiuping Fan,Chao Xu,Youwu He,Youfen Chen
Multidrug resistance (MDR) against chemotherapeutic agents has become the major obstacle to successful cancer therapy and multidrug resistance-associated proteins (MRPs) mediated drug efflux is the key factor for MDR. Indomethacin (IND), one of the non-steroidal anti-inflammatory agents, has been demonstrated to increase cytotoxic effects of anti-tumor agents as MRP substrates. In this study, dextran- g -indomethacin (DEX-IND) polymeric micelles were designed to delivery paclitaxel (PTX) for the treatment of MDR tumors. The DEX-IND polymer could effectively encapsulate PTX with high loading content and DEX-IND/PTX micelles present a small size distribution. Compared with free PTX, the release of PTX from DEX-IND/PTX micelles could be prolonged to 48 h. Cellular uptake test showed that the internalization of DEX-IND/PTX micelles by drug-sensitive MCF-7/ADR cells was significantly higher than free PTX benefiting from the inhibitory effect of IND on MRPs. In vitro cytotoxicity test further demonstrated that DEX-IND/PTX micelles could enhance the cytotoxicity of PTX against MCF-7/ADR tumor cells. In vivo pharmacokinetic results showed that DEX-IND/PTX micelles had longer systemic circulation time and slower plasma elimination rate in comparison to PTX. The anti-tumor efficacy test showed that DEX-IND/PTX micelles exhibited greater tumor growth-inhibition effects on MDR tumor-bearing mice, with good correlation between in vitro and in vivo. Overall, the cumulative evidence indicates that DEX-IND/PTX micelles hold significant promise for the treatment of MDR tumors.
研究领域:
肿瘤学
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药剂学
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生物医学工程
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DOI
PubMed
高影响因子
JOURNAL OF CONTROLLED RELEASE
·
2023
·
IF 10.8
Deqing Lin,Xiaoning Xu,Lin Chen,Lei Chen,Mengyun Deng,Jinrun Chen,Zhibin Ren,Lei Lei,Jiaqing Wang,Jie Deng,Xingyi Li
Herein, we report a facile method for converting carboxylate-containing indomethacin (Idm) into a cyclooxygenase-2 (COX-2) selective inhibitor via the amidation of an unnatural peptide sequence (Nal-Nal-Asp). The resulting indomethacin amides ( i.e., Idm-Nal-Nal-Asp) have high selectivity for COX-2, and can self-assemble into a one-component supramolecular hydrogel that acts as a ‘self-delivery’ system for boosting anti-inflammatory efficacy. Self-assembled Idm-Nal-Nal-Asp hydrogel robustly inhibits COX-2 expression in lipopolysaccharide (LPS)-activated Raw 264.7 macrophages while also exhibits superior anti-inflammatory and antioxidant activities via reactive oxygen species (ROS)-related NF-κB and Nrf2/HO-1 pathways. Moreover, a rabbit model of endotoxin-induced uveitis (EIU) reveals that the Idm-Nal-Nal-Asp hydrogel outperforms clinically used 0.1 wt% diclofenac sodium eye drops in terms of in vivo anti-inflammatory efficacy via topical instillation route. As a rational approach to designing and applying COX-2 selective inhibitors, this work presents a simple method for converting non-selective nonsteriodal anti-inflammatory drugs (NSAIDs) into highly selective COX-2 inhibitors that can self-assemble into supramolecular hydrogel for anti-inflammation applications.
研究领域:
药物化学
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材料科学
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生物医学工程
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药理学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2025
·
IF 5.2
Jiawei Han,Zhimin Yue,Wen Sun,Weitao Fang,Yunran Zhang,Xiaoqian Liu,Jue Wang,Jiaxin Chen
With the expansion of gel research, organic small molecule gels are beginning to gain attention. Whether the small-molecule gel approach can be a new formulation strategy of solubilization and permeation promotion for poorly soluble drugs needs to be explored in this study. The model ingredient indomethacin (IND) as a nonsteroidal anti-flammatory drug shows limited therapeutic application mainly due to its low water solubility. Herein, the IND small molecule hydrogel was design to co-formed with a small molecule ligand by integrating theory-model-experiment techniques. Then, the formed IND small molecule hydrogels (i.e., IND-MEG hydrogel and IND-ARG hydrogel) with meglumine (MEG) or arginine (ARG) appeared typical 3-D network with good rheology. In comparison to crystalline IND, the solubilities of IND-MEG hydrogel and IND-ARG hydrogel exhibited 506.71-fold and 479.63-fold improvements, respectively. Meanwhile, both IND hydrogels performed significantly enhanced release rate and degree, and maintained supersaturation for a long time arising from the complexation reaction of IND and ligand, which was revealed by phase solubility and fluorescence quenching studies. Furthermore, the designed IND hydrogels significantly promoted IND membrane permeability compared to the commercial IND hydrogel, and enhanced the development potential of novel IND hydrogels for oral and transdermal applications. Therefore, this study provides a new formulation technique to increase the solubility/release and permeability of poorly water-soluble drugs by designing their small molecule hydrogel systems.
研究领域:
药剂学
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药物化学
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产品关联
DOI
PubMed
高影响因子
DRUG DELIVERY
·
2022
·
IF 6.819
Jiangxiu Niu,Ming Yuan,Hongying Li,Yao Liu,Liye Wang,Yanli Fan,Yansong Zhang,Xianghui Liu,Lingmei Li,Jingxiao Zhang,Chenyu Zhao
Challenges associated with topical analgesics and anti-inflammatory drugs include poor drug penetration and retention at the desired lesion site. Therefore, improving these challenges would help to reduce the toxic and side effects caused by drug absorption into the systemic circulation and improve the therapeutic efficacy of topical therapeutic drugs. Pentapeptide (KTTKS) is a signal peptide in skin tissue, it can be recognized and bound by signal recognition particles. In the current study, we successfully prepared novel indomethacin (IMC) loaded KTTKS-modified ethosomes (IMC-KTTKS-Es), and the physicochemical properties and topical efficacy were investigated. Results showed that the prepared IMC-KTTKS-Es displayed a particle size of about 244 nm, a negative charge, good deformability, and encapsulation efficiency (EE) exceeding 80% for IMC, with a sustained release pattern. In vitro percutaneous permeation studies revealed that the skin retention was increased after the drug was loaded in the IMC-KTTKS-Es. Confocal laser scanning microscopy also showed improved skin retention of IMC-KTTKS-Es. In addition, IMC-KTTKS-Es showed improved topical analgesic and anti-inflammatory activity with no potentially hazardous skin irritation. This study suggested that the IMC-KTTKS-Es might be an effective drug carrier for topical skin therapy with a good safety profile.
研究领域:
药剂学
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皮肤生物学
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药物递送系统
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DOI
PubMed
高影响因子
AAPS PHARMSCITECH
·
2026
·Vol. 27
·期 3
·127
·
IF 5.1
Qu Jianlu,Jia Chaoliang,Chen Yaobin,Qu Haibin,Li Wenlong
In this study, a stable nanocrystalline drug delivery system for indomethacin (IND) was rapidly developed by integrating machine learning methods with Hummer Acoustic Resonance (HAR) technology. This system effectively enhanced the solubility of IND and demonstrated excellent scalability. High-throughput screening using HAR technology identified P188-PVA as the optimal composite stabilizer for IND nanocrystal suspensions. Molecular dynamics simulations were employed to thoroughly investigate the interaction mechanisms between the drug and stabilizers. Systematic design and optimization of IND nanocrystal formulation parameters and HAR process conditions were conducted using an integrated modeling approach combining Box-Behnken design (BBD) and artificial neural networks (ANN). Various statistical metrics were employed to evaluate and compare the predictive accuracy and generalization capability of BBD-RSM and ANN models, thereby identifying the optimal formulation. HAR technology was successfully used to scale up the optimal formulation by 5- and 50-fold, demonstrating its initial potential for scalability. Freeze-drying, spray-drying, and fluidized-bed drying techniques were evaluated for solidifying the prepared nanocrystal suspensions. Multiple analytical techniques were employed to characterize the particle size and solid-state properties of IND nanocrystals. PXRD and DSC analyses confirmed the crystalline nature of the IND nanocrystals. In vitro dissolution experiments indicated that IND nanocrystals exhibited significantly improved dissolution compared to raw IND. Additionally, the concepts and methodologies proposed in this study could also be applied to the development of other poorly water-soluble drugs. Graphical
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DOI
高影响因子
MOLECULES
·
2024
·Vol. 29
·期 5
·1055
·
IF 4.2
Jing Xu,Xiu-Wei Yang
Berberine is a natural isoquinoline alkaloid with low toxicity, which exists in a wide variety of medicinal plants. Berberine has been demonstrated to exhibit potent prevention of indomethacin-induced gastric injury (GI) but the related mechanism remains unclear. In the present study, liquid chromatography-mass spectrometry (LC-MS)-based metabolomics was applied for the first time to investigate the alteration of serum metabolites in the protection of berberine against indomethacin-induced gastric injury in rats. Subsequently, bioinformatics was utilized to analyze the potential metabolic pathway of the anti-GI effect of berberine. The pharmacodynamic data indicated that berberine could ameliorate gastric pathological damage, inhibit the level of proinflammatory factors in serum, and increase the level of antioxidant factors in serum. The LC-MS-based metabolomics analysis conducted in this study demonstrated the presence of 57 differential metabolites in the serum of rats with induced GI caused by indomethacin, which was associated with 29 metabolic pathways. Moreover, the study revealed that berberine showed a significant impact on the differential metabolites, with 45 differential metabolites being reported between the model group and the group treated with berberine. The differential metabolites were associated with 24 metabolic pathways, and berberine administration regulated 14 of the 57 differential metabolites, affecting 14 of the 29 metabolic pathways. The primary metabolic pathways affected were glutathione metabolism and arachidonic acid metabolism. Based on the results, it can be concluded that berberine has a gastroprotective effect on the GI. This study is particularly significant since it is the first to elucidate the mechanism of berberine’s action on GI. The results suggest that berberine’s action may be related to energy metabolism, oxidative stress, and inflammation regulation. These findings may pave the way for the development of new therapeutic interventions for the prevention and management of NSAID-induced GI disorders.
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产品关联
DOI
PubMed
高影响因子
Science of Advanced Materials
·
2015
·Vol. 7
·期 12
·2508-2514
·
IF 2.598
Zhong Suni,Chen Yanzhong,Song Fenyun,Tian Yong,Wang Xiufang
The synthesis of magnetic mesoporous carbon spheres (FeMCs) with sucrose, silica, and hydrated iron nitrite Fe(NO3)3 · 9H2O under neutral conditions was achieved by the ultrasonication method. Indomethacin (INC) was selected as the model drug.
FeMCs before and after INC-loading FeMCs were characterized by scanning electron microscopy (SEM), wide-angle X-ray diffraction (WXRD), nitrogen sorption isotherms, and differential scanning calorimetry (DSC). Release tests were conducted to confirm improvements in drug release kinetics. The
experimental results showed that the mesoporous carbon spheres exhibited BET surface areas of 615–876 m2/g and pore volumes of 1.36–2.25 cm3/g. INC showed an amorphous state after it was incorporated into the mesoporous channels of the FeMCs. Release kinetics
revealed that the release rate of INC from FeMCs was significantly higher than that of pure INC. This finding may be attributed to the reduced crystallinity of INC in the composites. FeMCs could be exploited as an alternative delivery system for poorly water-soluble indomethacin. The crystallinity
of the loaded drug and the drug release kinetics could be well controlled by FeMCs developed in this method.
研究领域:
材料科学
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药学
·
纳米技术
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DOI
高影响因子
RSC Advances
·
2017
·Vol. 7
·期 37
·22802-22809
·
IF 3.108
Ruobai Li,Jing Kong,Haijin Liu,Ping Chen,Guoguang Liu,Fuhua Li,Wenying Lv
The degradation of indomethacin (IM) by ferrous ion-activated potassium peroxydisulfate (Fe2+/PDS) was investigated. We aimed to determine the optimal conditions for the removal of IM under different concentrations of Fe2+and PDS, evaluate the effects of operational parameters (solution pH, humic acid (HA), N2 bubbling and persulfate species), and propose the degradation mechanism of IM by the Fe2+/PDS system. The sequential addition of Fe2+ led to an improvement in the IM degradation and TOC removal efficiency. When the molar ratio of IM/PDS/Fe2+ was 1 : 1.5 : 2, the IM was almost completely degraded. Restrictions to the degradation efficiency of IM were caused by increasing the solution pH, bubbling with nitrogen, or through the addition of HA. A low concentration of Cl− had no effect on the reaction, while a high concentration led to a dramatic inhibitory effect. In addition, quenching experiments revealed that SO4˙− was the major active radical for the degradation of IM by ferrous ion-activated peroxydisulfate. Based on the identification of transformation products by liquid chromatography-mass spectrometry (LC-MS/MS), the pathways of the ferrous–peroxydisulfate oxidative system for the degradation of IM were tentatively proposed.
研究领域:
环境科学
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化学工程
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DOI
高影响因子
International Journal of Nanomedicine
·
2017
·
IF 4.3
Yunfang Zhou,Shuanghu Wang,Xuhua Ying,Yifan Wang,Peiwu Geng,Aiping Deng,Zhihong Yu
Multidrug resistance (MDR) against chemotherapeutic agents has become one of the major obstacles to successful cancer therapy and MDR-associated proteins (MRPs)-mediated drug efflux is the key factor for MDR. In this study, a redox-responsive polymer based on dextran (DEX) and indomethacin (IND), which could reduce MRPs-mediated efflux of chemotherapeutics, was synthesized, and the obtained polymer could spontaneously form stable micelles with well-defined core-shell structure and a uniform size distribution with an average diameter of 50 nm and effectively encapsulate doxorubicin (DOX); the micelles contain a disulfide bridge (cystamine, SS) between IND and DEX (DEX-SS-IND). In vitro drug release results indicated that DEX-SS-IND/DOX micelles could maintain good stability in a stimulated normal physiological environment and promptly depolymerized and released DOX in a reducing environment. After incubating DEX-SS-IND/DOX micelles with drug-resistant tumor (MCF-7/ADR) cells, the intracellular accumulation and retention of DOX were significantly increased under the synergistic effects of redox-responsive delivery and the inhibitory effect of IND on MRPs. In vitro cytotoxicity showed that DEX-SS-IND/DOX micelles exhibited higher cytotoxicity against MCF-7/ADR cells. Moreover, DEX-SS-IND/DOX micelles showed significantly enhanced inhibition of tumor in BALB/c nude mice bearing MCF-7/ADR tumors and reduced systemic toxicity. Overall, the cumulative evidence indicates that DEX-SS-IND/DOX micelles hold significant promise for overcoming MDR for cancer therapy.
研究领域:
药学
·
肿瘤学
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DOI
高影响因子
Pharmaceuticals
·
2026
·Vol. 19
·期 6
·944
·
IF 5.7
Linhan Li,Jie Wang,Jie Xu,Jiaxin Li,Gang Jin
Objectives: To address the critical limitations of current formulations that fail to simultaneously resolve indomethacin’s poor water solubility, susceptibility to gastric acid hydrolysis, and difficulty in balancing rapid onset with long-term sustained release, this study prepared solid dispersions via anti-solvent freeze-drying to improve drug dissolution, constructed oral buccoadhesive bilayer controlled-release tablets using direct powder compression, and elucidated the intrinsic relationships among polymer gel properties, swelling-erosion behavior, tablet integrity maintenance, and drug release mechanisms.Methods: Solid dispersions (SDs) were prepared by anti-solvent freeze-drying. Bilayer tablets (25 mg IND/tablet, 12.5 mg/layer) were fabricated via direct powder compression after optimizing disintegrants and polymer matrices. In vitro dissolution, surface pH, adhesion time, and adhesion strength were evaluated.Results: SDs enhanced dissolution by at least 30-fold in water and 2.4-fold at pH 6.8 within 2 h versus pure drug. Optimized bilayer tablets achieved 45% drug release at 20 min and 80% sustained release over 8 h, with surface pH of 6.8 ± 0.1, adhesion time of 8.3 ± 0.1 h, and adhesion strength of 57 ± 0.13 g.Conclusions: The physicochemical properties of polymeric excipients are critical for balancing drug release and mucoadhesion in buccal tablets. To achieve ideal controlled-release effects, in addition to focusing on the swelling and erosion characteristics of matrix-based tablets, the ability to maintain tablet integrity during dynamic dissolution must be further investigated, which is an essential factor for ensuring precisely modulated drug release. Meanwhile, when employing solid dispersions as solubilizing intermediates to prepare controlled-release formulations, the gelling properties of polymers in each formulation component should be fully considered to avoid incomplete disintegration and insufficient release at the initial dissolution stage.
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DOI
PubMed
高影响因子
International Journal of Electrochemical Science
·
2023
·
IF 1.5
Yuxia Liu,Qing Huang,Cuizong Zhang,Caiyun Liang,Liyun Wei,Jinyun Peng
A novel method was described for sensitive voltammetric determination of indomethacin based on a graphene loaded nickel oxides nanoparticles (Gr-NiO) film by one-step electrodeposition. The as-prepared electrode (Gr-NiO/GCE) was characterized by electrochemical methods and scanning electron microscopy. The electrocatalytic properties of Gr-NiO/GCE toward the oxidation of indomethacin were analyzed via cyclic voltammetry (CV) and differential pulse voltammetry (DPV). The results indicate that the one-step prepared Gr-NiO/GCE can remarkably enhance electrocatalytic activity towards the oxidation of indomethacin. Under optimized conditions, voltammetric response of Gr-NiO/GCE was linear to indomethacin within the concentration range of 2.0×10 -7 -7.0×10 -5 mol L -1 , with the detection limit of 5.4×10 −8 mol L −1 (S/N=3). And, the method was also applied to detect indomethacin in pharmaceutical dosage forms with wonderful satisfactory.
研究领域:
分析化学
·
药物分析
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DOI
高影响因子
危险品化学品经营许可证（带存储）