Materials Science & Engineering C-Materials for Biological Applications
·
2015
·
IF 3.088
Jing Li,Lu Xu,Hongyu Wang,Baixue Yang,Hongzhuo Liu,Weisan Pan,Sanming Li
The purpose of this study was to facilely develop amino modified mesoporous silica xerogel synthesized using biomimetic method (B-AMSX) and to investigate its potential ability to be a drug carrier for loading poorly water-soluble drug indomethacin (IMC). For comparison, mesoporous silica xerogel without amino modification (B-MSX) was also synthesized using the same method. The changes of characteristics before and after IMC loading were systemically studied using fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), small angle X-ray scattering (SAXS) and nitrogen adsorption/desorption analysis. The results showed that B-MSX and B-AMSX were spherical nanoparticles with mesoporous structure. Compared with B-MSX, IMC loading capacity of B-AMSX was higher because more drug molecules can be loaded through stronger hydrogen bonding force. DSC and SAXS analysis confirmed the amorphous state of IMC after being loaded into B-MSX and B-AMSX. The in vitro drug release study revealed that B-MSX and B-AMSX improved IMC release significantly, and B-AMSX released IMC a little faster than B-MSX because of larger pore diameter of IMC-AMSX. B-MSX and B-AMSX degraded gradually in dissolution medium evidenced by color reaction and absorbance value, and B-AMSX degraded slower than B-MSX due to amino modification. In conclusion, B-AMSX with superiority of higher loading capacity and enhanced dissolution release can be considered to be a good candidate as drug carrier for IMC.
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MICROCHIMICA ACTA
·
2018
·Vol. 185
·期 8
·1-8
·
IF 5.705
Deng Ya’nan,Shen Jiwei,Liu Jiawei,Wei Yinmao,Wang Chaozhan
Poly(2-naphthyl acrylate) was first grafted onto silica-coated magnetic nanoparticles by surface-initiated atom transfer radical polymerization to prepare a reversed-phase magnetic adsorbent. The resulting polymer brush displays enhanced extraction efficiency by offering active sites on the surfaces of adsorbent. It was applied to the preconcentration of the non-steroidal antiinflammatory drugs (NSAIDs) indomethacin (InDo) and diclofenac (DIC). These drugs interact with the sorbent through hydrophobic and π-interactions, and via electrostatic attraction. By coupling the magnetic solid-phase extraction with HPLC, a method for analysis of InDo and DIC in the environmental water samples was established. The limits of detection range from 0.62 to 0.64 ng·mL −1 , and the relative standard deviations for intra-and inter-day analyses of spiked water samples are <11.9%, and relative recoveries are between 62.1 and 96.7%.
A reversed-phase magnetic adsorbent was prepared by grafting poly(2-naphthyl acrylate) brush on the surface of silica coated magnetic nanoparticles. Due to the two conjugated aromatic rings of the monomer, the polymer brush can effectively extract non-steroidal anti-inflammatory drugs through strong π- and hydrophobic interactions.
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TROPICAL JOURNAL OF PHARMACEUTICAL RESEARCH
·
2023
·Vol. 22
·期 1
·15-22
·
IF 0.6
Jingwen Gong,Yu Xie,Yinfen Tan,Hailong Li,Junqing Zhang
Purpose: To investigate the mechanism of action of galangin (GAL) against indomethacin (Indo)-induced gastric injury.
Methods: Ten micromolar GAL with 2 mM Indo or 0.5 mM L-NAME or 2 mM propargylglycine were co-administered to human gastric mucosal epithelial cells GES-1 for 24 h. Cell viability assay and reactive oxygen species (ROS) test were conducted with commercial kits. Protein expressions of constitutive and inducible nitric oxide synthase (cNOS and iNOS, respectively), and cystathionine-γ-lyase (CSE) in GSE-1 cells were investigated by western blot. After 100 - 300 mg/kg, GAL was daily administered to rats for 5 days, and 30 mg/kg Indo was administered to induce gastric injury. Protein expressions of endothelial NOS (eNOS), iNOS, CSE, nuclear factor (NF)-κB, PKC, Akt, phospho-eNOS (Ser-1177), and phospho-eNOS (Thr-495) were investigated by western blot.
Results: Galangin ameliorated the proliferative inhibitions of Indo, propargylglycine, and L-NAME on GSE-1 cells (p < 0.05), rapidly scavenged ROS, and increased cNOS protein expressions (p < 0.05). Galangin (300 mg/kg) inhibited protein expressions of iNOS (p < 0.01), NF-κB, Akt, and PKC (p < 0.05), inhibited the Ser-1177 and Thr 495 phosphorylation of eNOS, elevated eNOS and CSE protein expressions (p < 0.001).
Conclusion: Galangin protects gastric mucosa from Indo by scavenging ROS and inhibiting protein expressions of Akt and PKC. The inhibition leads to Ser-1177 and Thr 495 dephosphorylation of eNOS, thereby prolonging eNOS activity. Besides, GAL inhibits iNOS-produced NO by inhibiting NF-κB to ameliorate the inflammatory reaction induced by Indo.
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JOURNAL OF MOLECULAR STRUCTURE
·
2019
·
IF 2.12
Qiang Fu,Hai-Dong Lu,Yi-Fei Xie,Jia-You Liu,Yang Han,Ning-Bo Gong,Fang Guo
Indomethacin ( Indo ) and naproxen ( Nap ) belong to Biopharmaceutical Classification System (BCS) class II drugs, which permeate membranes well but are poorly soluble. Two pharmaceutical salts hydrate of Indo and Nap with (1R,2R)-1,2-diphenylethylenediamine ( DPEN ) were obtained using solution crystallization. Both salts, (DPEN) 2 ·(Indo) 2 ·(H 2 O) 2 and (DPEN) 1 ·(Nap) 1 ·(H 2 O) 0.5 , were characterised using various solid-state characterisation techniques such as single crystal X-ray diffraction (SCXRD), powder X-ray diffraction (PXRD), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), and Raman spectra . The structure analysis shows that DPEN is monocation as only one amine is protonated into ammonium. The Indo , DPEN and water molecules form one-dimensional hydrogen bond chains through extensive N H⋯O, N H⋯N and O H⋯N interactions. The solubility study shows that the two salts are more soluble in pH 1.2, 4.5 and 6.8 buffer mediums compared with pure raw materials. Solubility thermodynamics calculation was carried out to further understand the solubility properties of two salts.
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APPLIED CATALYSIS B-ENVIRONMENTAL
·
2017
·
IF 9.446
Fengliang Wang,Ping Chen,Yiping Feng,Zhijie Xie,Yang Liu,Yuehan Su,Qianxin Zhang,Yingfei Wang,Kun Yao,Wenying Lv,Guoguang Liu
In this study, a novel visible-light-driven N-doped carbon dot (NCDs)/g-C 3 N 4 composite was successfully synthesized by loading NCDs nanoparticles onto the interlayers and surface of g-C 3 N 4 via a facile polymerized method. The photocatalytic activity of the NCDs/g-C 3 N 4 was remarkably higher than that of g-C 3 N 4 and CDs/g-C 3 N 4 toward the degradation of indomethacin (IDM) under visible light irradiation. With increasing NCDs loading volumes, the photocatalytic activity of NCDs/g-C 3 N 4 initially increased, and then decreased. A very low NCDs content of 1.0 wt% resulted in a 13.6 fold higher reaction rate than that of pristine g-C 3 N 4 . This enhanced photocatalytic activity might have been ascribed to the unique up-converted PL properties, efficient charge separation, as well as bandgap narrowing of the NCDs. Reactive species (RS) scavenging experiments revealed that superoxide radical anions (O 2 −) and photogenerated holes (h + ) played key roles during the photocatalytic degradation of IDM. The quantification of O 2 − showed that NCDs/g-C 3 N 4 formed a larger amount of O 2 − than that of pristine g-C 3 N 4 . Potential photocatalytic pathways of IDM were proposed through the identification of intermediates using HPLC–MS/MS and the prediction of reaction sites based on Frontier Electron Densities (FEDs) calculations, which involved decarboxylation, hydroxylation, as well as the addition and cleavage of indole rings. Toxicity and mineralization evaluations revealed that NCDs/g-C 3 N 4 provided a very desirable performance for the toxicity reduction and mineralization of IDM under longer exposures of visible light irradiation.
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SEPARATION AND PURIFICATION TECHNOLOGY
·
2025
·
IF 9
Haijun Chen,Chunli Kang,Shiyi Zhao,Zhuowen Wang,Haiyang Liu,Deming Dong,Jiao Qu,Na Zheng,Xiuyi Hua
Ineffective separation of photo-carriers and slow photoreaction rates seriously limit the decontamination effectiveness of the photocatalyst. To overcome these limitations, herein, the oxygen vacancies modified Z-scheme Ag 3 PO 4 /FeSnO(OH) 5 heterojunction was designed with FeSnO(OH) 5 as a co-catalyst. In this photosystem, Ag 3 PO 4 and FeSnO(OH) 5 function as oxidation and reduction centers of Ag 3 PO 4 /FeSnO(OH) 5 photocatalysts, respectively. Importantly, oxygen vacancies in the Z-scheme heterojunction provide an effective charge transport pathway, which not only inhibits the photocorrosion of Ag 3 PO 4 but also reduces electron-hole recombination, significantly boosting the photocatalytic decontamination performance and long-term stability of the Ag 3 PO 4 /FeSnO(OH) 5 photocatalyst. Remarkably, the Ag 3 PO 4 /FeSnO(OH) 5 photocatalyst demonstrated outstanding photocatalytic performance, 100 % degrading indomethacin (IDM) under visible light in just 30 min through the main generation of h + that attacks the active atoms of IDM, prominently outperforming other counterparts. Besides, three principal degradation pathways were proposed, and the toxicity of the degradation products was significantly reduced. The Ag 3 PO 4 /FeSnO(OH) 5 exhibited high photocatalytic degradation efficacy across different qualities of water. This research offers an oxygen vacancy modified engineering combined with a Z-scheme heterojunction strategy for constructing extraordinary photocatalysts for environmental purification.
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MICROPOROUS AND MESOPOROUS MATERIALS
·
2020
·
IF 4.551
Jia Ke,Yumei Wang,Lingmei Wang,Baixue Yang,Kaijun Gou,Yanxin Qin,Sanming Li,Heran Li
A series of core-shell mesoporous silica nanoparticles (MSN@Ms) were successfully prepared with reducing response environmental stimuli TEOS-BTES as a shell and mesoporous silica nanoparticles (MSN) as a core. The results demonstrated that both MSN and MSN@Ms possessed spherical mesoporous structure and good porosity. Moreover, the size of particles and thickness of shell can be regulated by BTES amount. Besides, Indomethacin (IMC) could be loaded into the silica carriers in amorphous state, and the IMC loading amount was positively correlated with the pore volume . The release profile illustrated that the TEOS-BTES shell coating on the surface of MSN could act as reducing activatable trigger to achieve control release, while MSN provided enough space to encapsulate IMC with high loading. It was also found that MSN and MSN@Ms could be degraded in vitro. Furthermore, both IMC-MSN and IMC-MSN@M2 could reduce the gastric mucosa irritation and improve the bioavailability of IMC, and IMC-loaded MSN had a higher bioavailability than IMC-loaded MSN@M2.
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SEPARATION AND PURIFICATION TECHNOLOGY
·
2025
·
IF 9
Irfan Ijaz,Aysha Bukhari,Ammara Nazir,Ezaz Gilani,Hina Zain,Attia Shaheen,Mohammed Rafi Shaik,Mujeeb Khan
Designing effective adsorbents for adsorption of the threatening level of pharmaceuticals and personal care products (PPCPs) pollution is an immediate challenge for wastewater treatment. In the current work, molybdenum borides (MoBT x ) were first composited with silk fibroin (SF) through ultrasonic self-assembly. Then, the MoBT x @SF composite’s surface was modified with phytic acid (PA) to create MoBT x @SF@PA composite. The as-synthesized MoBT x @SF@PA adsorbent was developed to effectively remove indomethacin (IDM) and ceftriaxone (CEF). Due to the abundance of functional groups, highly exposed available active sites, and higher BET (Brunauer-Emmett-Teller) surface area (786.8 m 2 /g), MoBT x @SF@PA demonstrated an outstanding adsorption capability for IDM (549.89 mg/g) and CEF (959.18 mg/g), exceeding the earlier reported adsorbents. A kinetic study revealed that the interaction between the MoBT x @SF@PA adsorbent and PPCPs obeyed a pseudo-second-order model (PSO), implying that chemisorption controls the adsorption process. The Langmuir isotherm model and thermodynamic study indicated that IDM and CEF adsorption followed monolayer adsorption and were endothermic and spontaneous. Fourier-transformed infrared spectroscopy (FTIR) and X-ray photoelectron spectroscopy (XPS) were used to explore the adsorption mechanism. Multiple hydrogen bindings, electrostatic interactions, high surface area, and porosity of the composite were primarily responsible for remarkable adsorption capacity. These results highlight a versatile approach for MoBT x -based adsorbent preparation with exceptional adsorption qualities appropriate for real-world PPCPc-polluted wastewater treatment.
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Pharmaceutics
·
2020
·Vol. 12
·期 2
·144
·
IF 4.421
Ziyue Xi,Wei Zhang,Yali Fei,Mingshu Cui,Luyao Xie,Lu Chen,Lu Xu
This work explored absorption efficacy via an in vivo imaging system and parallel artificial membrane penetration in indomethacin (IMC) solid dispersion (SD) systems. Two different polymer excipients—hydroxypropyl methylcellulose (HPMC) and Kollicoat IR as precipitation inhibitors (PIs)—combined with mesoporous silica nanoparticles (MSNs) as carriers were investigated. The IMC–SDs were prepared using the solvent evaporation method and characterized by solubility analysis, infrared (IR) spectroscopy, powder X-ray diffraction (PXRD), field emission scanning electron microscopy (FESEM), and differential scanning calorimetry (DSC). It was confirmed that IMC successfully changed into an amorphous state after loading into the designed carriers. The in vitro release and stability experiments were conducted to examine the in vitro dissolution rates of IMC–SDs combined with HPMC and Kollicoat IR as PIs which both improved approximately three-fold to that of the pure drug. Finally, in vivo studies and in vitro parallel artificial membrane penetration (PAMPA) experiments ensured the greater ability of enhancing the dissolution rates of pure IMC in the gastrointestinal tract by oral delivery. In brief, this study highlights the prominent role of HPMC and Kollicoat IR as PIs in MSN SD systems in improving the bioavailability and gastrointestinal oral absorption efficiency of indomethacin.
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Journal of Pharmaceutical Analysis
·
2020
·
IF 2.673
Xuguang Zhang,Zhenrui Xie,Xun Chen,Junqiang Qiu,Yinfeng Tan,Xiaoliang Li,Hailong Li,Junqing Zhang
Alpinia officinarum Hance of the Chinese traditional herb for the treatment of emesis, abdominal pain and diarrhea has been used to counteract gastric disease induced by indomethacin in rats without obvious side effects. However, the role of herb-drug interaction between indomethacin and A. officinarum based on pharmacokinetic, tissue distribution and excretion still remains unknown. In this study, an ultra-fast liquid-tandem mass spectrometry (UFLC-MS/MS) method was developed for simultaneous determination of indomethacin and its three metabolites, O-desmethylindomethacin (ODI), deschlorobenzoylindomethacin (NDI) and indomethacin acyl-β-D-glucuronide (IDAβG) by oral administration of indomethacin solution with and without the ethanolic extract of A. officinarum and applied to comparative pharmacokinetic, tissue distribution and excretion studies. Our results clarified that oral administration of A. officinarum produced significant alterations in the pharmacokinetic parameters of indomethacin. And the pharmacokinetic interaction between indomethacin and A. officinarum reduced the systemic exposure of indomethacin and increased its elimination. Tissue distribution results demonstrated that co-administration of A. Officinarum could not reduce the accumulation of indomethacin in the target tissue of the stomach, but could accelerate the excretions of indomethacin and its three metabolites including ODI, NDI and IDAβG in the bile and feces of rats in the excretion study. Therefore, A. Officinarum might have a gastrointestinal protective effect through the interaction role with indomethacin based on the pharmacokinetics and excretion in rats.
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Nanoscale
·
2020
·Vol. 12
·期 15
·8546-8562
·
IF 6.895
Na Yin,Xinyi Tan,Hongbing Liu,Fengming He,Ning Ding,Jingxin Gou,Tian Yin,Haibing He,Yu Zhang,Xing Tang
Rheumatoid arthritis (RA) is an autoimmune disease characterized by inflammatory cell infiltration, and cartilage and bone disruption, which ultimately leads to loss of joint function. Current treatments for RA only focus on anti-inflammatory activity but neglect to prevent further damage to articular cartilage and bone. Here we attempted to co-deliver indomethacin (IND), methotrexate (MTX) and a small-interfering RNA targeting MMP-9 using an in situ hydrogel loaded with PEI-SS-IND-MTX-MMP-9 siRNA nanoparticles (D/siRNA-NGel) to treat RA synergistically and comprehensively. IND, MTX and MMP-9 siRNA were able to escape from the endosome and down-regulate the expression of MMP-9 and inflammatory cytokines of Raw-264.7 cells. After intra-articular injection in arthritic mice, the D/siRNA-NGel effectively relieved joint swelling and significantly reduced the expression of TNF-α, IL-6 and MMP-9 in the ankle fluid, knee joint fluid and plasma of RA mice without causing any side effects. Most importantly, the co-delivery system restored the morphological parameters of the ankle joints close to normal. The D/siRNA-NGel could achieve good anti-inflammatory activity and reverse cartilage disruption through a synergistic effect between chemical drugs and MMP-9 siRNA. This co-delivery system should have promising applications in the treatment of rheumatoid arthritis and other metabolic bone diseases which cause serious bone erosion.
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TOXICOLOGY AND APPLIED PHARMACOLOGY
·
2026
·
IF 3.6
Yangyi Huang,Jinfei Li,Yue Lu,Jie Cao,Xinzhi Wang,Hao Wu,Min Shen,Hongli Yu
A lectin from Pinellia ternata tubers (PTL, 12 kDa) with potent pro-inflammatory activity binds to the plasma membrane and translocates into the cytoplasm. However, its cellular entry route and inflammatory toxicity mechanisms remain unclear. Here, confocal microscopy showed that fluorescein isothiocyanate (FITC)-labeled PTL (50 μg/mL) accumulated on the cell surface and was endocytosed by RAW264.7 cells time-dependently. Pharmacological inhibition revealed that PTL uptake was mediated by the mannose receptor C-type 2 (MRC2) and predominantly via clathrin-mediated endocytosis. After endocytosis, PTL translocated to mitochondria with marked co-localization, inducing mitochondrial damage characterized by membrane potential dissipation, calcium overload, and excessive mitochondrial reactive oxygen species (mtROS) generation. These alterations promoted intracellular ROS accumulation and amplified inflammatory responses. Co-immunoprecipitation with mass spectrometry identified ATP synthase subunit beta (ATP5B) as a mitochondrial interacting protein of PTL. Their interaction was validated by molecular docking, co-localization, and microscale thermophoresis (MST). ATP5B knockdown markedly attenuated PTL (50 μg/mL)-induced ROS production, inflammatory cytokine expression, and mitochondrial injury, indicating ATP5B is a critical mediator of PTL's inflammatory toxicity. Collectively, these findings demonstrate that PTL induces mitochondrial damage and pro-inflammatory responses in RAW264.7 cells through MRC2-mediated, clathrin-dependent endocytosis and subsequent ATP5B interaction. This study establishes a mechanistic link between lectin endocytosis, mitochondrial targeting, and inflammatory toxicity, providing new insight into plant lectin-mediated immunotoxicity.
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