International Journal of Electrochemical Science
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2023
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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.
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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.
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ACS Biomaterials Science & Engineering
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2022
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IF 5.395
Chunlu Wang,Yaoyao Zheng,Yaxin Zheng,Can Wu,Xiujie Wang,Menghua Huang,Xiaoxing Wu,Wenying Zhong,Keming Xu
Non-steroidal anti-inflammatory drugs (NSAIDs) have drawn considerable attention in the field of cancer treatment, yet these drugs display limited potency and selectivity against cancer cells. To address these problems, we designed a peptide-based self-delivery system [Indomethacin-Phe-Phe-Tyr (H2PO3)-Ser-Val, IDM-FFpYSV] that combines an NSAID molecule (indomethacin, or IDM) and a segment of anticancer tripeptide (tyroservatide, or YSV). IDM-FFpYSV is capable of self-assembling in an aqueous solution to afford nanofibrillar hydrogels under the catalysis of alkaline phosphatases (ALPs), which are overexpressed on the plasma membrane of cancer cells. The IDM-FFpYSV + ALP hydrogel displays a continuous release profile of peptide drugs, whereas a solution mixture of pure drugs (IDM-OH + pYSV + ALP) shows burst release of drug moieties. The treatment of IDM-FFpYSV selectively inhibits the proliferation of HeLa cells in vitro, with precise regulations of intracellular targeting proteins (COX-2 and AC-H3). The enhanced potency and selectivity of IDM-FFpYSV are found to be attributed to enhanced cellular uptake of peptide drugs, which involves a caveolae-mediated endocytosis pathway. Furthermore, intravenous administration of the IDM-FFpYSV formulation significantly inhibits the tumor growth in a HeLa-xenografted mouse model, whereas treatment of solution mixtures of pure drugs (IDM-OH + pYSV) fails to do so. Taken together, the study provides a viable strategy to augment anticancer efficacies of self-delivery system through molecular integration of multiple anticancer elements with an enzyme-instructed self-assembly process.
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JOURNAL OF DRUG TARGETING
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2019
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IF 3.277
Chen Yang,Yu Zhang,Peng Cai,Shirui Yuan,Qiaofang Ma,Ya Song,Haobo Wei,Ziheng Wu,Zhenghong Wu,Xiaole Qi
Generally, definite intestine targeting and immediate drug releasing are both important for the treatment of colon cancer via oral administration of anti-cancer drugs. We developed a highly specific oral colon-targeted pulsatile capsule, based on the effective enzyme-responsive ‘pulse plug’, which can be degraded under mannanase abundant in colon. Indomethacin (IN) solid dispersion immediate-release pellets were filled in an insoluble capsule body, a guar gum-lactose-hydroxypropyl methylcellulose (HPMC) composed tablet was embedded on the top of capsule as the ‘pulse plug’, and then covered by enteric soluble cap. In this study, the influence of the proportion of guar gum/lactose/HPMC, the viscosity of HPMC, and the tablet weight on the degradation behaviour of the plug tablet was investigated. The drug-releasing profiles of those pulsatile capsules in different simulated colon medium verified the ‘pulse plug’ could realise the colon-targeted pulsatile drug-releasing. Furthermore, the rabbit pharmacokinetic experiments showed that the in vivo time lag of drug loaded pulsatile capsules was significantly extended to 5.61 ± 0.08 h (p<.01), compared with that (0.33 ± 0.47 h) of the marketed tablets (YUNPENG®). These results indicated that colon-targeted pulsatile capsules would be effective oral delivering system for colon cancers therapy.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2025
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IF 8.5
Irfan Ijaz,Aysha Bukhari,Ammara Nazir,Ezaz Gilani,Hina Zain,Attia Shaheen,Mohammed Rafi Shaik,Mujeeb Khan
Lowering the threat of antibiotics is a hot issue in environmental chemistry. To overcome this problem, a novel MBene-based adsorbent, DTT@BC@MoBT x , was designed by modification of bacterial cellulose (BC) using MoBT x MBene and 1,4-dithiothreitol (DTT). Several characterization methods, including Fourier transforms infrared (FTIR), X-ray photoelectron spectroscopy (XPS), and X-ray Diffraction (XRD), confirmed the successful synthesis of DTT@BC@MoBT x composite. It was discovered that the abundance of functional groups, higher specific surface area, and porosity were facilitative for DTT@BC@MoBT x adsorbents to indomethacin (IDM) and losartan (LP). The adsorption of IDM and LP well fitted to the pseudo-second-order kinetic model and Langmuir isotherm model, suggesting the single-layer chemisorption occurred on the adsorbent. The maximum sorption capabilities of the DTT@BC@MoBT x adsorbent were 1041.26 mg/g for IDM and 887.31 mg/g for LP, indicating excellent adsorption performance. The adsorption capacities of IDM and LP showed a slight decline after four consecutive adsorption-desorption tests, indicating excellent regeneration ability and stability. Interfering monoanionic (Na + and K + ) and monoanionic (Cl − and NO 3 − ) exhibited negligible impacts on IDM and LP elimination rates at all three concentrations. Additionally, it was discovered that metal ions had a greater ability for interference in a higher valency state (Mg 2+ , Ca 2+ , SO 4 2− , and CO 3 2− ) than in a lower valency state (Na + , K + , Cl − , and NO 3 − ). The adsorption processes of IDM and LP by the DTT@BC@MoBT x adsorbent involved hydrogen bonding and electrostatic attraction, as shown by FTIR and XPS analyses. This work offered a novel MBene-based adsorbent for the quick and effective adsorption of IDM and LP from water.
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INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2009
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IF 3.061
Jianyu Xin,Zhizhang Guo,Xingyu Chen,Wenfeng Jiang,Jianshu Li,Maolin Li
A series of branched cationic β-cyclodextrin polymers (CPβCDs) with designed chemical structures were synthesized from β-cyclodextrin (β-CD), epichlorohydrin (EP) and choline chloride (CC). Indomethacin (IDM), an anionic drug, was chosen as a model drug to evaluate the drug loading capacities of CPβCDs. The formation of IDM-CPβCD complex was confirmed by 1 H NMR and DSC . Phase solubility studies and Job plots indicated that CPβCDs can solubilize IDM up to 100 times of its intrinsic solubility in a 1:1 complexation form. Mechanism studies with the help of adamantane revealed that the effective complexation is a combination of inclusion complexation, charge interaction and hydrophobic interaction. In addition, IDM-CPβCDs loaded alginate hydrogels were prepared and obtained controllable release profile in dissolution tests. The tunable structures of CPβCDs make them promising drug carriers with superior drug loading capacities and controllable drug release abilities.
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Journal of Materials Chemistry B
·
2019
·Vol. 8
·期 5
·993-1007
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IF 5.047
Na Yin,Xueting Guo,Rong Sun,Hongbing Liu,Lihua Tang,Jingxin Gou,Tian Yin,Haibing He,Yu Zhang,Xing Tang
Rheumatoid arthritis is a chronic systemic autoimmune disease that causes joint swelling and cartilage damage. The objective of the present work was to develop a temperature-sensitive hydrogel (D-NGel) containing nanoparticles (D-NPs), which could simultaneously deliver combination indomethacin and methotrexate. D-NPs were formed by multiple non-covalent interactions between PEI-SS and the carboxyl-containing hydrophobic small molecule drugs IND and MTX, which were then loaded into a temperature-sensitive hydrogel matrix. The Tsol/gel of the temperature-sensitive hydrogel matrix composed of 27% F127 and 10% F68 was 33 °C and the gelation time was less than 15 s. The resultant D-NGel was injected into the articular cavity of collagen-induced arthritis rats and quickly transformed in situ into gels which slowly released drug in the joint fluid for up to 72 h. The D-NGel effectively reduced joint swelling, bone erosion and expression of inflammatory cytokines in the ankle fluid and knee joint fluid. In addition, liver and kidney function tests and histopathological examination indicated there was a good biological safety for D-NGel. In conclusion, this work has demonstrated the great potential of the D-NGel for sustained co-delivery of IND and MTX for the synergistic treatment of rheumatoid arthritis, treating both the symptoms and the root causes of rheumatoid arthritis.
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DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
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2025
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IF 2.2
Wenhui Zhou,Mengmeng Han,Haosen Zhang,Tianwei Zhang,Haiyun Tian,Tingting Yang,Tao Liu
Objective This study investigated the effect of molecular interactions between drug and polymers on preparation of nanoamorphous indomethacin (IND) through milling of solid dispersions (SDs).Significance The polymer selection (molecular interaction) emerged as a critical factor in the dynamic milling process for achieving nanoamorphous drug.Methods Polyvinylpyrrolidone (PVP) and hydroxypropyl methylcellulose (HPMC) were selected as models. Amorphous dispersions were used to prepare nanoamorphous drugs by applying wet milling. Molecular simulations were employed to elucidate the molecular mechanisms of drug–polymer miscibility, interaction energy, and molecular migration.Results Both PVP and HPMC related SDs could be nanosized after milling. The rate of size reduction might be related to the solid state of the dispersions. The combination of amorphous PVP SDs with reduced particle size significantly improved the dissolution rate of IND. However, HPMC-based samples exhibited recrystallization during milling. Molecular simulation indicated that PVP formed strong molecular interaction with the drug to maintain the amorphous form, which contributed to avoid recrystallization induced by the external milling forces. The radial distribution function of hydrated IND/HPMC amorphous cells demonstrated the absence of hydrogen bonding interactions between IND and HPMC.Conclusion PVP contributed to maintain the amorphous state during the milling process, which resulted from the higher molecular binding energy compared to HPMC. Controlled milling of amorphous SD with optimized polymer selection could simultaneously achieve nanoamorphous particle and enhanced dissolution rate.
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COLLOIDS AND SURFACES B-BIOINTERFACES
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2025
·
IF 5.6
Jianlu Qu,Changhao Jia,Xiaoyang Zhang,Wenlong Li
Indomethacin (IND) is a nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic properties, and is widely used for the treatment of diverse inflammatory diseases. However, its poor aqueous solubility severely limits its clinical application. An orally dissolving film (ODF) loaded with an indomethacin solid dispersion (IND-SD) was developed to enhance dissolution. Based on Hansen solubility parameters (HSP), four polymers were selected to prepare the IND-SD, and the optimal carrier and drug to polymer ratio were identified by in vitro dissolution testing. Molecular docking and molecular dynamics (MD) simulations were employed to elucidate drug-polymer interactions at the molecular level. Under the guidance of Quality by Design (QbD), an optimization framework integrating a Box-Behnken design (BBD) and an artificial neural network (ANN) was established to design and optimize the ODF formulation. Multiple statistical metrics were used to assess the Box-Behnken design response surface methodology (BBD-RSM) model and the ANN model, with the ANN model demonstrating superior predictive accuracy in predicting the film critical quality attributes (CQAs). PXRD and DSC analyses confirmed that IND existed in an amorphous state in both the IND-SD and the ODF. In vitro dissolution experiments demonstrated that the cumulative drug release from the ODF in simulated saliva within 1 min was significantly higher than that of pure IND and IND-SD.
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Chinese Journal of Integrative Medicine
·
2026
·
IF 3.1
Hou Yu-jun,Wang Wen,Ye Jiang-nan,Wang Lu,Zhou Si-yuan,Shi Yun-zhou,Chen Ying,Yao Jun-peng,Sun Lu-qiang,Li Ying
Objective To compare the effectiveness of electroacupuncture (EA) combined with omeprazole (Ome) and Ome alone on indomethacin-induced gastric injury mice and reveal the underlying mechanism of this combination. Methods Fourty-eight male C57BL/6J mice were randomly divided into 6 groups by a simple random method ( n =8), including control, model, Ome, Ome + EA, Ome + sham EA, and Ome + EA + ML385 groups. A gastric ulcer mouse model was constructed by intragastrically administering indomethacin at a dose of 30 mg/kg. EA and Ome treatment were performed twice daily with each session of EA treatment lasting 20 min. Gastric injury severity was determined by measuring the ulcer index. Sixteen mice with gastric ulcers underwent left cervical vagotomy (CV) were further divided into model + CV and Ome + EA + CV groups. Eight mice with gastric ulcers underwent sham vagotomy and EA combined with Ome treatment were included in the Ome + EA + SCV group. Following respective treatments, the gastric mucosal ulcer tissues were collected and pathologic scores were evaluated by HE staining. Oxygenase-1/tumor necrosis factor-α levels in gastric tissue were measured using ELISA. Colorimetric assay was conducted to measure oxidative stress levels. Real-time polymerase chain reaction was applied to detect the expression of nuclear factor erythroid 2-related factor 2 (Nrf2) in gastric tissue. Immunofluorescence staining was performed to observe the locations and expressions of F4-80 and Nrf2 in the gastric mucosa. CV was conducted to evaluate the role of the vagus nerve in EA-mediated gastric injury improvement. Results EA combined with Ome alleviated gastric ulcers and decreased gastric pathologic scores (both P <0.01). Furthermore, it decreased gastric oxidative stress levels and inhibited macrophages activation (all P <0.01). However, vagotomy abolished the antioxidant function of EA. Meanwhile, we observed that Nrf2 plays a critical role in inducing the therapeutic effect of EA combined with Ome on gastric injury. Conclusion In mice with gastric ulcers, EA combined with Ome can better repair indomethacin-induced gastric injury via inactivation of macrophages and Nrf2-mediated antioxidant signaling pathway, which is primarily mediated by vagus nerve.
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Drug Delivery and Translational Research
·
2023
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IF 5.4
Liu Jie,Lin Chenshi,Wu Man,Wang Yingjie,Chen Shenyu,Yang Taiwang,Xie Chenlu,Kong Yue,Wu Wenliang,Wang Jiaping,Ma Xiaonan,Teng Chao
Uric acid is the final metabolite in humans. High level of uric acid chronically induces urate deposition, aggravates kidney damage, and concomitantly causes an increase in inflammatory factors. Alleviating acute inflammation and decreasing uric acid levels are the key points in the treatment of inflammatory diseases associated with high uric acid. However, a drug delivery system that combines anti-inflammatory and uric acid reduction functions at the same time remains a challenge to be settled. Here, we designed a nanocrystal-based co-delivery platform, IND Nplex, characterized by loading of indomethacin (IND) and uricase. Compared with free IND or uricase, IND Nplex possessed a better anti-inflammatory effect by restraining the release of inflammation-related factors in vitro. In addition, pharmacokinetic and biodistribution studies revealed that IND Nplex significantly prolonged the retention time in vivo and was more concentrated in the kidney. In acute gouty arthritis model rats, IND Nplex markedly relieved ankle joint swelling and mitigated synovial inflammation. In acute kidney injury model rats, IND Nplex indicated better biocompatibility and significant amelioration of renal fibrosis. Moreover, IND Nplex showed the effect of anti-inflammatory and improved renal function via determination of inflammatory factors and biochemical markers in the serum and kidney. In conclusion, these results indicate that IND Nplex exerts anti-inflammatory activity and uric acid–lowering effect and could become a promising candidate for the treatment of uric acid–related diseases. Graphical Abstract
In this study, a stable neutral co-delivery platform (IND Nplex) was fabricated by using a co-delivery strategy, allowing for a combination of the anti-inflammation drug IND and the metabolic enzyme uricase. IND Nplex showed a good therapeutic effect on rats with acute gouty arthritis or acute kidney injury due to the dual effects of anti-inflammatory and uric acid lowering. This platform provided a novel strategy for high uric acid–related illnesses.
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ChemPlusChem
·
2014
·Vol. 79
·期 5
·725-731
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IF 3.242
Jiali Gao,Qing Li,Wenshuai Chen,Yixing Liu,Haipeng Yu
Graphical Long-lasting effects : A hierarchical structure of cellulose nanofibers and indomethacin has been fabricated through self-assembly and recrystallization under the combined effects of solvent and processing method (see figure). Such hybrid films possess a high loading capacity and encapsulation efficiency, and show a sustained drug release period over 30 days. Cellulose nanofibers (CNFs) were isolated from poplar wood by using a mild chemical pretreatment combined with a high-intensity ultrasonication method. The as-prepared CNFs were used as a template to load indomethacin (IMC). With the nucleation and growth of IMC on the surfaces of CNFs and CNF clusters, CNF/IMC composite fibers were eventually fabricated. The effects of solvent and processing method on the structures of the composite fibers were analyzed in terms of morphology, surface charge, and crystal form. Drug-release characteristics of the composite fibers were evaluated by dissolution tests, in which the drug-releasing curves of the composite fibers were fitted to a mathematical model describing the releasing kinetics. The experimental results demonstrated that the composite fibers possessed an encapsulation efficiency of up to 97 %, and a sustained drug-release period of over 30 days.
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