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POLYMER · 2016 · IF 3.586

Dual pH and oxidation-responsive nanogels crosslinked by diselenide bonds for controlled drug delivery

Xinfeng Cheng,Yong Jin,Rui Qi,Wuhou Fan,Hanping Li,Xiaopeng Sun,Shuangquan Lai

A new diselenide crosslinked polyurethane nanogel was developed, which could respond to pH change and oxidaiton condition. Firstly, PEGylated polyurethane (MPEG-PUBM-MPEG) containing tertiary amino and Br groups was prepared, which can assemble into micelles in aqueous solution. Then the nanogels with diselenides crosslinked polyurethane (PU) core and hydrophilic PEG shell were prepared using sodium diselenide (Na 2 Se 2 ) as a crosslinking agent to react with the Br groups in the PUBM block. The resultant nanogels exhibited enhanced colloidal stability relative to the non-crosslinked micelles, which have a spherical morphology with a diameter about 110–120 nm. Interestingly, the nanogels displayed a pH-induced swelling and oxidation-triggered dissociation behaviors, which can efficiently load indomethacin (IND) drugs and showed an inhibited premature release behavior as compared to the non-crosslinked micelles. An accelerated release behavior at pH 5.0 (54% in 24 h) and a burst release under oxidation condition (95% in 20 h) were observed for the nanogels, indicating their dual pH and oxidation-triggered release behaviors. Considering their enhanced stability, pH-induced swelling and oxidation-triggered degradation characteristics, the diselenide crosslinked nanogels can serve as a potential system for controlled drug delivery.

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RSC Advances · 2015 ·Vol. 5 ·期 120 ·99418-99424 · IF 3.84

Preparation and characterization of N-phthaloyl-chitosan-g-(PEO–PLA–PEO) as a potential drug carrier

Jinda Fang,Ke Zhang,Jingwei Jia,Zhengke Wang,Qiaoling Hu

To improve the drug-loading capacity and control the initial release of amphiphilic drug carriers, a series of N-phthaloyl-chitosan-g-(PEO–PLA–PEO) compounds were synthesized with well-defined structures. The self-assembly behavior of copolymers in aqueous solutions was confirmed by various techniques such as fluorescence spectrometry, dynamic light scattering, and transmission electron microscopy. The results demonstrated that the micellization behavior of graft copolymers was different from that of their linear counterparts. The micelle sizes of the graft copolymers could be tuned with chemical composition as well as temperature. Furthermore, when hydrophobic indomethacin was loaded into the micelles, the graft copolymer micelles trapped more indomethacin than PEO–PLA–PEO micelles, facilitating the in vitro control of the initial burst release of the drug. Drug release could be controlled in vitro by simply altering the EO/LA ratio of the grafting chains. The graft copolymer showed low cytotoxicity to 293T cells, indicating its great potential application for drug delivery.

CAS / MDL: 53-86-1 129-00-0
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BIOMACROMOLECULES · 2013 · IF 5.371

In Situ Controlled Release of rhBMP-2 in Gelatin-Coated 3D Porous Poly(ε-caprolactone) Scaffolds for Homogeneous Bone Tissue Formation

Qingchun Zhang,Ke Tan,Yan Zhang,Zhaoyang Ye,Wen-Song Tan,Meidong Lang

In tissue engineering, incorporation of bone morphogenetic protein-2 (BMP-2) into biomaterial scaffolds is an attractive strategy to stimulate bone repair. However, suboptimal release of BMP-2 remains a great concern, which may cause unfavorable bone formation as well as severe inflammation. In this study, genipin-cross-linked gelatin entrapped with recombinant human BMP-2 (rhBMP-2) was exploited to decorate the interior surface of three-dimensional porous poly(ε-caprolactone) (PCL) scaffolds. With gelatin-coating, PCL scaffolds demonstrated enhanced water uptake and improved compressive moduli. Intriguingly, a unique release profile of rhBMP-2 composed of a transient burst release followed by a sustained release was achieved in coated scaffolds. These coated scaffolds well supported growth and osteogenesis of human mesenchymal stem cells (hMSCs) in vitro, indicating the retaining of rhBMP-2 bioactivity. When hMSCs-seeded scaffolds were implanted subcutaneously in nude mice for 4 weeks, better bone formation was observed in gelatin/rhBMP-2-coated scaffolds. Specifically, the spatial distribution of newly formed bone was more uniform in gelatin-coated scaffolds than in uncoated scaffolds, which displayed preferential bone formation at the periphery. These results collectively demonstrated that gelatin-coating of porous PCL scaffolds is a promising approach for delivering rhBMP-2 to stimulate improved bone regeneration.

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EUROPEAN POLYMER JOURNAL · 2013 · IF 2.562

Preparation and drug release property of CO2 stimulus-sensitive poly(N, N-dimethylaminoethyl methacrylate)-b-polystyrene nanoparticles

Xiaohong Wang,Guohua Jiang,Zhen Wei,Xia Li,Bolin Tang

The CO 2 stimulus-sensitive nanoparticles based on poly( N , N -dimethylaminoethyl methacrylate)- b -poly styrene (PDMAEMA- b -PS) were prepared via surfactant-free miniemulsion reversible addition–fragmentation chain transfer (RAFT) polymerization. The as-prepared nanoparticles exhibited core–shell structure with about 120   nm in diameter. Their dispersion/aggregation in water can be adjusted by alternatively bubbling of CO 2 and N 2 . Drug release from these nanoparticles can be accelerated (or delayed) by bubbling (or removing) of CO 2 .

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LANGMUIR · 2013 · IF 4.187

Electrospun Upconversion Composite Fibers as Dual Drugs Delivery System with Individual Release Properties

Zhiyao Hou,Xuejiao Li,Chunxia Li,Yunlu Dai,Ping’an Ma,Xiao Zhang,Xiaojiao Kang,Ziyong Cheng,Jun Lin

Novel multifunctional poly(ε-caprolactone)-gelatin encapsulating upconversion core/shell silica nanoparticles (NPs) composite fibers as dual drugs delivery system (DDDS), with indomethacin (IMC) and doxorubicin (DOX) releasing in individual release properties, have been designed and fabricated via electrospinning process. Uniform and monodisperse upconversion (UC) luminescent NaYF4:Yb3+, Er3+ nanocrystals (UCNCs) were encapsulated with mesoporous silica shells, resulting in the formation of core/shell structured NaYF4:Yb3+, Er3+@mSiO2 (UCNCs@mSiO2) NPs, which can be performed as DOX delivery carriers. These UCNCs@mSiO2 NPs loading DOX then were dispersed into the mixture of poly(ε-caprolactone) (PCL) and gelatin-based electrospinning solution containing IMC, followed by the preparation of dual drug-loaded composite fibers (DDDS) via electrospinning method. The drugs release profiles of the DDDS were measured, and the results indicated that the IMC and DOX released from the electrospun composite fibers showed distinct properties. The IMC in the composite fibers presented a fast release manner, while DOX showed a sustained release behavior. Moreover, the UC luminescent intensity ratios of 2H11/2/4S3/2–4I15/2 to 4F9/2–4I15/2 from Er3+ vary with the amounts of DOX in the system, and thus drug release can be tracked and monitored by the luminescence resonance energy transfer (LRET) mechanism.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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TALANTA · 2015 · IF 3.545

Preparation, characterization and application of a reversed phase liquid chromatography/hydrophilic interaction chromatography mixed-mode C18-DTT stationary phase

Qing Wang,Yao Long,Lin Yao,Li Xu,Zhi-Guo Shi,Lanying Xu

A mixed-mode chromatographic stationary phase , C18-DTT (dithiothreitol) silica (SiO 2 ) was prepared through “thiol-ene” click chemistry. The obtained material was characterized by fourier transform infrared spectroscope, nitrogen adsorption analysis and contact angle analysis. Chromatographic performance of the C18-DTT was systemically evaluated by studying the effect of acetonitrile content, pH, buffer concentration of the mobile phase and column temperature. It was demonstrated that the novel stationary phase possessed reversed phase liquid chromatography (RPLC)/hydrophilic interaction liquid chromatography (HILIC) mixed-mode property. The stop-flow test revealed that C18-DTT exhibited excellent compatibility with 100% aqueous mobile phase. Additionally, the stability and column-to-column reproducibility of the C18-DTT material were satisfactory, with relative standard deviations of retention factor of the tested analytes (verapamil, fenbufen , guanine , tetrandrine and nicotinic acid) in the range of 1.82–3.72% and 0.85–1.93%, respectively. Finally, the application of C18-DTT column was demonstrated in the separation of non-steroidal anti-inflammatory drugs, aromatic carboxylic acids , alkaloids, nucleo-analytes and polycyclic aromatic hydrocarbons . It had great resolving power in the analysis of various compounds in HILIC and RPLC chromatographic conditions and was a promising RPLC/HILIC mixed-mode stationary phase.

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JOURNAL OF CHROMATOGRAPHY A · 2015 · IF 4.169

Preparation, chromatographic evaluation and application of adenosine 5′-monophosphate modified ZrO2/SiO2 stationary phase in hydrophilic interaction chromatography

Qing Wang,Zhi-Yuan Luo,Mao Ye,Yu-Zhuo Wang,Li Xu,Zhi-guo Shi,Lanying Xu

The zirconia-coated silica (ZrO 2 /SiO 2 ) material was obtained by coupling layer-by-layer (LbL) self-assembly method and sol–gel technology, to take dual advantages of the suitable porous structure of SiO 2 and basic resistance of ZrO 2 . Adenosine 5′-monophosphate (5′-AMP) was then self-assembled onto ZrO 2 /SiO 2 via Lewis acid–base interaction, generating 5′-AMP-ZrO 2 /SiO 2 . The chromatographic properties of 5′-AMP-ZrO 2 /SiO 2 were systemically studied by evaluating the effect of acetonitrile content, pH and buffer concentration in the mobile phase. The results demonstrated that the 5′-AMP-ZrO 2 /SiO 2 possessed hydrophilic interaction chromatographic (HILIC) property comprising hydrophilic, hydrogen-bonding, electrostatic and ion-exchange interactions. For basic analytes, the column efficiency of ZrO 2 /SiO 2 and 5′-AMP-ZrO 2 /SiO 2 was superior to the bare ZrO 2 , and different selectivity was obtained after the introduction of 5′-AMP. For acidic analytes, good resolution was obtained on 5′-AMP-ZrO 2 /SiO 2 while the analysis failed on the bare ZrO 2 column owing to strong adsorption. Hence, the proposed 5′-AMP-ZrO 2 /SiO 2 had great potential in analyzing acidic compounds in HILIC mode. It was an extended application of ZrO 2 based SP.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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NUTRITION RESEARCH · 2015 · IF 2.472

Myricetin suppresses differentiation of 3 T3-L1 preadipocytes and enhances lipolysis in adipocytes

Qian Wang,Shuang-ting Wang,Xin Yang,Pan-pan You,Wen Zhang

Myricetin (MyR), a naturally occurring flavonol widely distributed in fruits, vegetables, and medicinal plants , has anticancer, anti-inflammatory, antihyperlipidaemic , and antiobesity activities. In the present study, we hypothesized that the antiobesity property of MyR is mediated via suppression of differentiation of preadipocytes into adipocytes and promotion of lipolysis of mature adipocytes, which effectively decrease the intracellular triglyceride concentration of adipocytes. Accordingly, the aim of this work was to investigate the effects of MyR on adipocyte differentiation and lipolysis in differentiated 3 T3-L1 adipocytes. Our results showed that MyR inhibited differentiation of 3 T3-L1 preadipocytes in a concentration-dependent manner. Myricetin downregulated the mRNA and protein levels of CCAAT/enhancer-binding protein α and peroxisome proliferator-activated receptor γ , both of which are major adipogenic transcription factors. Furthermore, the mRNA levels of other adipogenesis-related transcription factors, namely, CCAAT/enhancer-binding protein β , sterin regulatory element binding protein 1-c, peroxisome proliferator-activated receptor γ coactivator–1, adipocyte protein 2 , lipoprotein lipase and glucose transporter 4 , were also reduced by MyR treatment. Moreover, MyR significantly inhibited the phosphorylation of extracellular signal–regulated kinase, Jun N-terminal kinase, and p38 during the differentiation process. On the other hand, MyR induced a dose-dependent increase in glycerol release in fully differentiated adipocytes, indicating its stimulatory effect on adipocyte lipolysis. Furthermore, MyR downregulated mRNA level of perilipin A and enhanced the phosphorylation level of extracellular signal–regulated kinase, Jun N-terminal kinase, and p38 during lipolysis. Taken together, these findings indicate that MyR exerts antiobesity activity in adipocytes.

CAS / MDL: 28822-58-4 53-86-1
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ANALYTICAL AND BIOANALYTICAL CHEMISTRY · 2017 ·Vol. 409 ·期 12 ·3103-3113 · IF 3.431

Preparation of magnetic melamine-formaldehyde resin and its application to extract nonsteroidal anti-inflammatory drugs

Xue Shu-Wen,Li Jing,Xu Li

Magnetic melamine-formaldehyde resin was prepared via water-in-oil emulsification approach by entrapping Fe 3 O 4 magnetic nanoparticles as the core. The preparation of the magnetic resin was optimized by investigating the amount of polyethylene glycol 20000 and Fe 3 O 4 nanoparticles, the concentration of the catalyst (hydrochloric acid), as well as the mechanical stirring rate. The prepared material was characteristic of excellent anion-exchange capacity, good water wettability, and proper magnetism. Its application was demonstrated by magnetic solid-phase extraction of nonsteroidal anti-inflammatory drugs coupled to high performance liquid chromatography-UV analysis. Under the optimal conditions, the proposed method showed broad linear range of 1–5000 ng mL –1 of milk and urine samples, satisfactory reproducibility with intra-day and inter-day relative standard deviations less than 12.4% and 9.7%, respectively, and low limits of detection of 0.2 ng mL –1 for the studied nonsteroidal anti-inflammatory drugs. The developed method was successfully used for the determination of the nonsteroidal anti-inflammatory drugs in spiked urine and milk samples. The magnetic melamine-formaldehyde resin was promising for the sample pretreatment of acidic analytes via anion-exchange interaction with convenient operation from complex sample matrix. Magnetic solid-phase extraction based on melamine-formaldehyde resin

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JOURNAL OF MEMBRANE SCIENCE · 2024 · IF 8.4

Enhancing PPCP and salt separation in polyamide nanofiltration membranes with polydopamine and ZnO functionalized nanofiber support

Yuting Liu,Yinyu Chen,Huiying Ding,Jingchuan Xue,Yang Yang,Xianhui Li

Achieving the removal of pharmaceuticals and personal care products (PPCPs) while selectively rejecting divalent cations like Ca 2 ⁺ and Mg 2 ⁺ without compromising water productivity and recovery remains a challenge for existing commercial nanofiltration (NF) membranes used in drinking water treatment. These challenges stem from the limited pore size and insufficient negatively charged surface density of conventional NF membrane. This study employed a polydopamine-coated nanofibrous membrane, uniformly embedded with in-situ grown ZnO nanoparticles, as a porous support layer. In the interfacial polymerization process, the fabricated substrate regulated the diffusion of aqueous monomers, thereby optimizing the polyamide layer on composite NF membrane with thinner thickness, stronger surface density, crumple structure and appropriate pore size. This resulting membrane demonstrated excellent PPCP rejection while maintaining high permeability to essential minerals. Under optimal conditions, the designed membrane achieved an impressive water flux at about 21 L m⁻ 2  h⁻ 1  bar⁻ 1 and showed significant selectivity for PPCP and divalent cation, with diclofenac sodium rejection exceeding 90 % and Ca 2 ⁺ rejection of below 20 %. The incorporation of ZnO nanoparticles enlarged the active filtration surface and created additional water pathways, resulting in a water permeation rate that was double that of a pristine NF membrane, without compromising PPCP/divalent cation selectivity. This work provides valuable insights and important correlations for developing NF membranes aimed at enhancing water production while preserving selectivity for PPCP/divalent cation.

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EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS · 2024 · IF 4.4

Efficient cocrystal coformer screening based on a Machine learning Strategy: A case study for the preparation of imatinib cocrystal with enhanced physicochemical properties

Xiaoxiao Liang,Shiyuan Liu,Zebin Li,Yuehua Deng,Yanbin Jiang,Huaiyu Yang

Cocrystal engineering, which involves the self-assembly of two or more components into a solid-state supramolecular structure through non-covalent interactions, has emerged as a promising approach to tailor the physicochemical properties of active pharmaceutical ingredient (API). Efficient coformer screening for cocrystal remains a challenge. Herein, a prediction strategy based on machine learning algorithms was employed to predict cocrystal formation and seven reliable models with accuracy over 0.890 were successfully constructed. Imatinib was selected as the model drug and the models established were applied to screen 31 potential coformers. Experimental verification results indicated RF-8 is the optimal model among seven models with an accuracy of 0.839. When the seven models were combined for coformer screening of Imatinib, the combinational model achieved an accuracy of 0.903, and eight new solid forms were observed and characterized. Benefiting from intermolecular interactions, the obtained multicomponent crystals displayed enhanced physicochemical properties. Dissolution and solubility experiments showed the prepared multicomponent crystals had higher cumulative dissolution rate and remarkably improved the solubility of imatinib , and IM-MC exhibited comparable solubility to Imatinib mesylate α form. Stability test and cytotoxicity results showed that multicomponent crystals exhibited excellent stability and the drug-drug cocrystal IM-5F exhibited higher cytotoxicity than pure API.

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JOURNAL OF ETHNOPHARMACOLOGY · 2024 · IF 4.8

Elucidation of anti-pneumonia pharmacodynamic material basis and potential mechanisms of Xiebai San by combining spectrum–efficacy relationship and surface plasmon resonance

Anyi Zhao,Jiangmin Su,Qingxia Xu,Jun Zhang,Jinzhu Jiang,Sha Chen,Jintang Cheng,Chang Chen,Lianmei Wang,Jipeng Di,Xianju Liu,Liang Jiang,Li Liu,Yan Liu,An Liu,Cong Guo

Ethnopharmacological relevance Xiebai San (XBS), a classic Chinese prescription, has been used for the clinical treatment of pneumonia-related diseases for thousands of years. However, the anti-pneumonia pharmacodynamic material basis of XBS and its underlying mechanisms remain unclear. Aim of the study This study aimed to comprehensively investigate and verify the anti-pneumonia pharmacodynamic material basis and mechanisms of XBS. Materials and methods This study explored the anti-pneumonia activity and key pneumonia targets of XBS in lipopolysaccharide (LPS)-induced zebrafish and RAW264.7 cells in vivo and in vitro through transcriptomics, western blotting, and reverse transcription–quantitative polymerase chain reaction (RT–qPCR). The chemical fingerprint of XBS was established using high-performance liquid chromatography, and the similarities and areas of characteristic peaks of 15 batches of XBS were analyzed. Based on the spectrum–efficacy relationship, the potential anti-inflammatory components were screened according to their peak areas and efficacy using principal component analysis (PCA), bivariate correlation, and partial least squares regression analysis. Active components that bind to core targets were further screened based on surface plasmon resonance (SPR). The binding mode of proteins and components was simulated via molecular docking, which enabled the identification of the primary active components of XBS, thereby elucidating its anti-pneumonia properties. Finally, the anti-inflammatory activities of these components were verified in vitro . Results XBS decreased neutrophil aggregation in zebrafish and nitric oxide (NO) secretion in RAW264.7 cells as well as suppressed the release of downstream inflammatory cytokines such as iNOS, TNF-α, IL-1β, IL-18, and CXCL10 related to TNF and JAK–STAT signaling pathways. The phosphorylation of IκBα, Akt, and Stat3 was alleviated after XBS in cells. The fingerprint similarities of 15 batches of XBS ranged from 0.381 to 0.994, with a large difference. A total of 15 characteristic peaks were identified, and the relative standard deviation of their peak areas ranged from 24.1% to 70.7%. The results of in vitro anti-inflammatory activities of 15 batches of XBS showed that all samples inhibited the expression levels of NO and nine inflammatory markers. The anti-inflammatory index of 15 batches of XBS was determined to be 0.69–0.96 based on transformation of the anti-inflammatory rate and composite index method via PCA. The spectrum–efficacy relationship model of 15 characteristic peak areas and the anti-inflammatory index showed that 7 main potential active components were related to the anti-inflammatory activity of XBS. Moreover, four components (mulberroside A, isoquercitrin, liquiritigenin, and glycyrrhizic acid) screened based on SPR had different affinities toward TNFR1, Akt1, and Stat3 proteins, and the binding modes were elucidated via molecular docking. Finally, in LPS-induced RAW264.7 cells, all four active components (at a concentration of 60 μM) significantly inhibited the expression levels of NO and inflammatory markers. Conclusions Based on the comprehensive strategy of spectrum–efficacy relationship and SPR, mulberroside A, isoquercitrin, liquiritigenin, and glycyrrhizic acid were identified as the primary pharmacodynamic active components involved in the anti-pneumonia activity of XBS and were found to intervene in TNF and JAK–STAT signaling pathways.

CAS / MDL: 53-86-1 9004-67-5
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