DRUG DELIVERY
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2021
·
IF 6.419
Jianbo Li,Tiange Feng,Weijing Yang,Yaru Xu,Shuaishuai Wang,Huijie Cai,Zhilei Liu,Hong Qiang,Jinjie Zhang
Although Fraxinellone (Frax) isolated from Dictamnus albus L. possessed excellent anti-hepatic fibrosis activity, oral administration of Frax suffered from the inefficient therapeutic outcome in vivo due to negligible oral absorption. At present, the oral formulation of Frax is rarely exploited. For rational formulation design, we evaluated preabsorption risks of Frax and found that Frax was rather stable while poorly dissolved in the gastrointestinal tract (78.88 μg/mL), which predominantly limited its oral absorption. Further solubility test revealed the outstanding capacity of cyclodextrin derivatives (CDs) to solubilize Frax (6.8–12.8 mg/mL). This led us to study the inclusion complexes of Frax with a series of CDs and holistically explore their drug delivery performance. Characterization techniques involving 1H-NMR, FT-IR, DSC, PXRD, and molecular docking confirmed the most stable binding interactions when Frax complexed with 6-O-α-D-maltosyl-β-cyclodextrin (G2-β-CD-Frax). Notably, G2-β-CD-Frax exhibited the highest solubilizing capacity, fast dissolution rate, and superior Caco-2 cell internalization with no obvious toxicity. Pharmacokinetic studies demonstrated markedly higher oral bioavailability of G2-β-CD-Frax (5.8-fold that of free drug) than other Frax-CDs. Further, long-term administration of G2-β-CD-Frax (5 mg/kg) efficiently inhibited CCl4-induced hepatic fibrosis in the mouse without inducing any toxicity. Our results will inspire the continued advancement of optimal oral Frax formulations for anti-fibrotic therapy.
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PubMed
高影响因子
Food Bioscience
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2021
·
IF 4.24
Kehong Hou,Yaoyao Xu,Kaiyue Cen,Chengcheng Gao,Xiao Feng,Xiaozhi Tang
Essential oils (EOs) are gaining great interest as alternatives to synthetic food preservatives due to their antimicrobial activity . However, EOs are hydrophobic and easy to evaporate. In this research, EOs were encapsulated in nanoemulsions with the aid of hydroxypropyl-β-cyclodextrin (HPCD) to protect the ingredients and sustain the release, so as to exert long-term antibacterial effects. The influence of HPCD and its concentration on cinnamon essential oil (CEO) nanoemulsion formation, antibacterial activity , release property and stability was investigated. The results showed that HPCD reduced the particle size of nanoemulsion as the concentration of Tween 80 ranged from 2 to 4 g/L. However, HPCD addition showed adverse effect as the content of Tween 80 was 5 g/L. Antibacterial tests against Escherichia coli and Staphylococcus aureus demonstrated that the addition of HPCD contributed to the increase of antimicrobial activity of CEO nanoemulsions and showed the best effect when the concentration of HPCD was 30 g/L. The release experiment proved the slow-release ability of HPCD, and showed that the cavity of HPCD helped to reduce the loss of CEO, thus delayed the release time and enhanced the antibacterial effect. Meanwhile, the use of HPCD contributed to the storage stability of the emulsion at 4, 25, and 40 °C, and the nanoemulsion remained stable during a storage period of 60 days.
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高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2021
·
IF 5.875
Wenjing Su,Nikolay E. Polyakov,Wenhao Xu,Weike Su
This research aimed to overcome the current challenges in the application of natural carotenoid antioxidants, such as their complex preparation processes, low bioavailability and poor drug stability. Herein, a mechanochemical method was used to prepare an inclusion complex (IC) that self-assembles into micelles in aqueous solution and achieves solid-phase loading of astaxanthin (AST). The NMR analysis, thermodynamics study, particle size analysis and electron microscopy image results showed that AST, hydroxypropyl β-cyclodextrin (HPβ-CD) and glyceryl monostearate (GMS) formed self-assembled micelles and maintained good stability in aqueous solution. The antioxidant performance experiments showed that the formation of IC increases free radical scavenging activity. The pharmacokinetic studies showed that the bioavailability of the astaxanthin inclusion complex increased 4-fold. The tissue distribution experiments showed that the astaxanthin inclusion complex targets the liver to exert its antioxidant effects. The proposed method uses an innovative preparation technology to produce an efficient drug delivery system without solvents, and it exerts powerful antioxidant activity against astaxanthin.
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DOI
PubMed
高影响因子
SEPARATION AND PURIFICATION TECHNOLOGY
·
2021
·
IF 7.312
Jian Zhang,Yahui Liu,Wensen Liu,Lina Wang,Jing Chen,Zhaowu Zhu,Tao Qi
The synergisms of β-diketone and phosphine oxide are very efficient for lithium selective extraction from alkaline systems, and have been obtained wide applications, especially for lithium recovery from salt lake brines. However, the systems are ready to form emulsification which seriously impacted their practical applications. In this study, the synergistic mechanism of β-diketone and phosphine oxide was intensively studied using a typical β-diketone of HTTA (2-Thenoyltrifluoroacetone) and TOPO (Trioctylphosphine oxide) through extraction parameter relationships, FT-IR measurements, structure computational simulations. It is found that one molar water readily presented in the extracted species forming Li·(H 2 O)·TTA·TOPO, while two molar water presented when HTTA alone was used which more readily forms emulsification or even solid. When TOPO was attended, one molar of water was replaced by it as there is an unconfirmed “boundary“ formed between them which will significantly mitigate the emulsification formation.
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高影响因子
ENERGY & FUELS
·
2019
·
IF 3.021
Songjie Hua,Yuqi Hu,Liang Zhao,Liyuan Cao,Xiaoqin Wang,Jinsen Gao,Chunming Xu
For the effective removal of thiophene, a novel surface molecularly imprinted polymer (SMIP/MA@PCNS) was fabricated using porous carbon nanospheres (PCNS-5) as the support matrix and maleic acid (MA) as the functional monomer. Benefiting from the special amphiphilic properties of β-cyclodextrin as the carbon source, PCNS-5 exhibited good dispersion, uniform nanoscale sphere, and high specific surface area, which favored the rapid adsorption rate. Based on the intermolecular hydrogen bonds existing between carboxylic acid functional groups and thiophene, adsorption performances of different unsaturated polycarboxylic acids were investigated systematically. The results revealed that the optimal functional monomer was MA instead of the conventional methacrylic acid. Accordingly, SMIP/MA@PCNS was successfully applied to the direct removal of thiophene in the oil, reaching remarkable sulfur adsorption capacity (22.6 mg S g–1) within 120 min. Moreover, SMIP/MA@PCNS could selectively remove thiophene (16.2 mg S g–1) in the presence of structural analogues (3-methylthiophene, benzene, and cyclopentane) and exhibited an excellent regenerability with nice structural ability. These results indicated that SMIP/MA@PCNS possessed great promise in the desulfurization field.
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高影响因子
APPLIED SURFACE SCIENCE
·
2019
·
IF 5.155
Shu-ao He,Wei Li,Xiao Wang,Qiong Ma,Min Li,Wei Xu,Xue-chuan Wang,Chen-hui Zhao
The two-dimensional (2D) g-C 3 N 4 has a wide application prospect in photocatalysis field due to its larger surface reactions, wider absorption of light and faster charge separation. However, the lack of active site of reduction leads to its poor hydrogen evolution reaction (HER) activity. In this work, the intermediate β-FeOOH was synthesized as a high-efficiency precious metal free co-catalyst in hydrogen production. Then, the g-C 3 N 4 -Fe 3 O 4 /β-FeOOH (CNFF-x,y, x = 1, 2 and 3, y denotes the reaction time (h)) photocatalyst based on p-n and Z-scheme heterojunction was constructed via a subsequent solvothermal process. The chemical composition, microtopography, crystallography, photochemical and electrochemical properties of the CNFF-x,y were analyzed by XRD, FI-IR, TEM, XPS and so on. The visible-light-driven (VLD) catalytic performance of CNFF-x,y heterojunction was evaluated by the hydrogen evolution reaction (HER). Results showed that CNFF-2,10 photocatalyst based on p-n (g-C 3 N 4 -Fe 3 O 4 ) and Z-scheme (Fe 3 O 4 /β-FeOOH) heterojunction presented the highest VLD catalytic HER activity (33.25 μmol g −1 h −1 ) at the absence of Pt co-catalyst after illumination for 6 h. It indicated that the effective introduction of Fe 3 O 4 /β-FeOOH nanoparticles (NPs) into g-C 3 N 4 to construct double-heterojunction (g-C 3 N 4 -Fe 3 O 4 /β-FeOOH) could greatly broaden the light response property and inhibit the recombination of photo-induced carriers, exhibiting enhanced HER activity. Meanwhile, this double-heterojunction photocatalyst presented robust photostability and reproducibility even been used several times. The findings of an intermediate β-FeOOH were put forward in this study will provide some new ideas for the research of HER.
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高影响因子
REACTIVE & FUNCTIONAL POLYMERS
·
2019
·
IF 3.074
Liqin Zhou,Qinghua Liang,Kungang Chai,Zhangfa Tong,Hongbing Ji
To separate acetophenone (AP) and 1-phenylethanol (PE), a kind of cost-effective β-cyclodextrin based polymeric sorbent (CE-CDP) was constructed by crosslinking β-cyclodextrin with toluene-2,4-diisocyanate trimer. According to the characteristic results, the structure of the CE-CDP consisting of β-cyclodextrin cavity, aromatic urethane bond and unique isocyanurate ring was proved substantially. It was shown that crosslinking process would enhance the thermal stability, and the incorporation of the unique crosslinking units into CE-CDP's network potentially improved the selective adsorption performance compared to analogous polymer with non-isocyanurate ring structure. The static adsorption performance of CE-CDP in single solute system was investigated. The adsorption capacity of AP was much higher than that of PE, indicating that CE-CDP exhibits much stronger affinity toward AP over PE. Based on the results, we found that the spontaneous adsorption processes of AP and PE onto CE-CDP could be well described by pseudo-second order kinetics , Langmuir and Freundlich isotherm models. And the preferential AP adsorption over PE (selectivity≈6) was further verified through binary competitive adsorption. In addition, the density functional theory calculations showed that the coexistence of β-cyclodextrin cavity, aromatic urethane bond and isocyanurate ring endows CE-CDP with high AP adsorption capacity and selectivity. The theoretical results also indicated that the noncovalent interactions involving the intermolecular hydrogen bonding , π-π interactions and electrostatic interaction are favorable for binding AP rather than PE. In conclusion, CE-CDP was proved to be a good adsorbent for selective separation of AP and PE with mass producibility, low cost, high reusability and wide application prospect.
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Analytical Methods
·
2019
·Vol. 11
·期 42
·5398-5404
·
IF 2.378
Shengting Zhang,Mingrui Li,Dongbo Liu,Kunhao Qin,Yingying Xiang,Xiuling Ji,Congwen Li,Yunlin Wei
The human purinergic P2Y1 receptor (P2Y1R) belongs to the family of G-protein coupled receptors (GPCRs). Two stable cell lines, hP2Y1R-tGFP/U2OS and hP2Y1R-β-AR2-tGFP/U2OS, were generated with steady expression of fluorescent tGFP tagged P2Y1R or tGFP tagged β-arrestin2. The High Content Screening (HCS) technique was used to investigate P2Y1R mediated signal transduction processes based on the distribution of fluorescent receptors or the β-arrestin2/receptor complex. All procedures including aggregation, endolysis and resensitization that were involved in the interaction between the P2Y1 receptor and its ligand can be visualized using the tGFP labeled receptor combined with HCS technology in this study. ADP activated P2Y1R to induce a distinguished pattern of fluorescent vesicle formation inside both cell types. These two cell lines produced different peak fluorescence signals when activated by ADP at 100 μM, and the time to form the maximal vesicles was detected as 15 and 20 min respectively. The EC50 values of the concentration–response curves of ADP induced formation of fluorescent vesicles were 35.7 nM and 71.8 nM respectively. The ADP effects could be blocked by a P2Y1R specific antagonist MRS2179. The P2Y1R are coupled to Gq protein to activate PLC first, PLC cleave PIP2 into IP3 and DAG. And then DAG and Ca2+ activate PKC pathway, and finally the phospholipase D initiates β-arrestin2 mediated signal pathway. It took 30 and 45 min to complete P2Y1R re-sensitization in these two constructs respectively. Our results demonstrated that P2Y1R triggered downstream responses not only via heterotrimeric Gq proteins but also through β-arrestin2.
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高影响因子
TALANTA
·
2019
·
IF 4.916
Tingting Wang,Yuhuan Cheng,Yulian Zhang,Jinyin Zha,Jiannong Ye,Qingcui Chu,Guifang Cheng
In recent years, quantum dots (QDs) have attracted a tremendous amount of attention due to their compelling features. In this work, a kind of composite QDs based on β-cyclodextrin (β-CD) and its derivatives modification was prepared, and for the first time utilized to separate and determine enantiomers in the combined system of capillary electrophoresis with laser-induced fluorescence detection (CE-LIF). By taking advantages of the inclusion complexation of β-CD and the fluorescence property of QD core, the composite QDs were added into the running buffer as pseudo-stationary phase. The resultant CE-LIF method accomplished enantioseparation for six groups of model analytes without need of capillary preparation and analyte derivatization . The effects of composite QDs concentration, the pH value and concentration of the running buffer on resolution have been investigated individually. The RSDs of interday and intraday repeatability were in the range of 2.7–8.1%, 0.7–3.9%, and 1.5–3.8% for the peak area, migration time and resolution, respectively. The theoretical calculation results of the binding energies and binding constant further validated the interaction mechanism of composite QDs and target analytes. Furthermore, this developed method was successfully applied to the analysis of the active components (catechin and epicatechin) in Chinese herb Catechu , and the recoveries were in the range of 92.2–108%. The experimental results suggested that the preparation strategy of the composite QDs is appropriate for enantioseparation of more enantiomers by adjusting the modifiers on the surface of QDs, which is particularly promising for electrophoretic enantioseparation based on fluorescence detection, especially for those analytes lacking proper derivative functional groups.
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高影响因子
Asian Journal of Pharmaceutical Sciences
·
2019
·
IF 4.016
Shuying Li,Ying Zhang,Abdur Rauf Khan,Shuwang He,Yingxin Wang,Jiangkang Xu,Guangxi Zhai
The bitterness of a drug is a major challenge for patient acceptability and compliance, especially for children. Due to the toxicity of medication, a human taste panel test has certain limitations. Atomoxetine hydrochloride (HCl), which is used for the treatment of attention deficit/hyperactivity disorder (ADHD), has an extremely bitter taste. The aim of this work is to quantitatively predict the bitterness of atomoxetine HCl by a biosensor system. Based on the mechanism of detection of the electronic tongue (E-tongue), the bitterness of atomoxetine HCl was evaluated, and it was found that its bitterness was similar to that of quinine HCl. The bitterness threshold of atomoxetine HCl was 8.61 µg/ml based on the Change of membrane Potential caused by Adsorption (CPA) value of the BT0 sensor. In this study, the taste-masking efficiency of 2-hydroxypropyl-β-cyclodextrin (HP-β-CyD) was assessed by Euclidean distances on a principle component analysis (PCA) map with the SA402B Taste Sensing System, and the host–guest interactions were investigated by differential scanning calorimetry (DSC), powder X-ray diffraction (XRD), nuclear magnetic resonance (NMR) spectroscopy and scanning electron microscopy (SEM). Biosensor evaluation and characterization of the inclusion complex indicated that atomoxetine HCl could actively react with 2-hydroxypropyl-β-cyclodextrin.
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高影响因子
JOURNAL OF SEPARATION SCIENCE
·
2019
·Vol. 42
·期 6
·1248-1256
·
IF 2.516
Chengjun Wang,Lidong Cheng,Lin Zhang,Yuegang Zuo
Graphene oxide based molecularly imprinted polymers modified with β -cyclodextrin were prepared as solid-phase extraction column sorbents for specific recognition and sensitive detection of di(2-ethylhexyl) phthalate in water samples. The morphology and composition of synthesized sorbents were characterized by scanning electron microscopy, thermo-gravimetric analysis, Raman spectroscopy, and Fourier-transform infrared spectroscopy. The conditions affecting the performance of extraction procedures such as desorption solvent types and volume, sample pH and volume were investigated. The loading capacity (8.2 μg/mg) of the prepared sorbents increased eight times after modification with β -cyclodextrin. The developed extraction procedures coupled to high-performance liquid chromatography exhibited good linearity (0.2–500 μg/L), low limit of detection (0.052 μg/L), and good precision (relative standard deviation˂5.7%) under optimized conditions. The developed solid-phase extraction technique with prepared sorbents has been successfully applied in extracting trace di(2-ethylhexyl) phthalate from real natural waters with high efficiency, good selectivity, and desirable recoveries.
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PubMed
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Advanced Therapeutics
·
2019
·Vol. 2
·期 5
·1800136
·
IF 0
Yalu Zou,Yuanyuan Wang,Shengsheng Zhang,Yuntang Wu,Xiaofei Liu
Islet β cell failure is a critical metabolic disorder in the development of type 2 diabetes (T2DM), and the decreased viability and dysfunction of β cells accelerate diabetic pathogenesis in association with higher mortality. In this study, the therapeutic effects of chitooligosaccharide biguanide (COSG), which is similar in structure to metformin and has negligible side effects, on islet β-cell dysfunction and the possible mechanism are explored. Streptozocin-induced diabetic rats are administered COSG via daily intragastric gavage for 8 weeks. COSG significantly controlled body weight loss, attenuated glucose levels in blood and urine, and increased serum insulin. Histological examination of the pancreas reveals that COSG also alleviated pancreatic atrophy in T2DM rats. Furthermore, COSG stimulated insulin receptor substrate-2 (IRS-2) signaling in rat islet β cells, thereby mediating the activation of the phosphatidylinositol 3 kinase/protein kinase (PI3K/Akt) signaling pathway. In addition, COSG promoted downstream forkhead transcription factor O1 (FoxO1) nuclear output to potentially activate pancreas duodenum homeobox-1 (PDX-1)/glucose transporter type-2 (GLUT-2)/glucose kinase (GCK) pathway-regulated insulin secretion. COSG also inhibited the glycogen synthase kinase-3β (GSK-3β)/caspase-3 pathway to prevent cell apoptosis. The intrinsic protective effects of COSG on the impaired insulin signaling system to delay β-cell apoptosis, increase β-cell growth and proliferation, improve β-cell function and promote insulin secretion highlight the possibilities of COSG as a novel strategy for the prevention of T2DM.
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