JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2021
·
IF 3.981
Qikang Tian,Qianqian Han,Xin Zhu,Lan Zhang,Kun Chen,Zhishen Xie,Pan Wang,Xiangxiang Wu,Zhenqiang Zhang,Huahui Zeng
Celastrol is a promising drug candidate for treating diet-induced obesity, but the cytotoxicity and poor water solubility limit its clinical application. We prepared a novel celastrol conjugate (Cel-CMCS) with excellent water solubility (33.94 mg/mL), and then investigated its anti-obesity and toxic activities in diet-induced obese mice. Just as the parent celastrol, Cel-CMCS reduced body weight and body fat mass in an equally effective manner, but with lower toxicity. Collectively, Cel-CMCS provides a possible solution for the treatment of obesity in humans. In addition, the present study provided a practical experience of the development of carboxymethyl chitosan-based delivery system for poorly water-soluble drugs.
研究领域:
药学
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生物医学
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DOI
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
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2016
·
IF 1.78
Yanlei Kang,Jianming Gu,Xiurong Hu
Febuxostat was investigated due to its significant effect in the treatment of gout. However, its poor water solubility hinder its potential applications. In recent years, cocrystals have increasingly being applied to enhance the drug solubility . To improve the solubility, two cocrystals of Febuxostat were synthesized through the method of cooling crystallization. The prepared cocrystals febuxostat-isonicotinamide(FEB-INA) and febuxostat-arginine(FEB-Arg) were studied by microscopical observation, Powder X-Ray Diffraction(PXRD), Single Crystal X-ray Diffraction, Differential Scanning Calorimetry(DSC), and infrared spectrometry . At the same time, the cocrystals' solubility and dissolution rate were explored. Both the cocrystals showed higher solubility compared to the pure drug. The FEB-Arg cocrystal enhanced about 900 times of solubility compared to the pure drug. The current study proved that cocrystallization can be a better way to enhance the solubility of the poorly water-soluble drug.
研究领域:
药物化学
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材料科学
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药剂学
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DOI
高影响因子
MICROCHIMICA ACTA
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2019
·Vol. 186
·期 3
·1-9
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IF 5.479
Mutuyimana Félicité Pacifique,Liu Juanjuan,Nsanzamahoro Stanislas,Na Min,Chen Hongli,Chen Xingguo
The authors describe a one-step method for the preparation of yellow fluorescent carbon dots (CDs) starting from 4-aminoacetanilide hydrochloride and 4-acetamidobenzaldehyde. The CDs have excitation/emission peaks at 470/550 nm, good water solubility, salt-tolerance and photostability. Their fluorescence is quenched by hexavalent chromium [Cr(VI)] via static quenching. Fluorescence intensity drops linearly in the 1 to 400 μM Cr(VI) concentration range, and the limit of detection is 0.13 μM. This method is selective for Cr(VI) over potential metal ion interferences and was successfully applied to the detection of Cr(VI) in spiked water and biological tissue samples. Recoveries from spiked samples ranged from 97.7% to 103.8%.
Schematic presentation of ( a ) the preparation of the CD fluorescent probe and ( b ), the principle of Cr(VI) determination
研究领域:
分析化学
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环境科学
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DOI
PubMed
高影响因子
Canadian Journal of Chemistry
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2016
·Vol. 94
·期 6
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IF 1.003
Yafei Guo,Jiuling Li,Yuqi Liu,Yongping Ma,Huilin Cheng,Bo Yang,Dandan Liu,Rui Yang
This article describes the preparation of a series of inclusion complexes of anhydrolycorine with three cyclodextrins (CDs), namely β-CD, γ-CD, and 2-hydroxypropyl-β-cyclodextrin (HP-β-CD), and their successful characterization through UV, TG, DSC, XRD, SEM, 1H NMR, and 2D NMR spectroscopies. The results demonstrated that the water solubility of anhydrolycorine increased notably by about 23–42 times after the inclusion complexation with these CDs. Furthermore, preliminary in vitro cytotoxicity experiments on human colon cancer cell lines HT-29, SW480, HCT116, and DLD-1 were also performed, and the complexes showed remarkable anticancer activity against HT-29, SW480, and HCT116. These results suggested that the inclusion complexes would be potentially useful for applications for human colon cancer chemotherapy.
研究领域:
药学
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肿瘤学
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有机化学
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DOI
高影响因子
MATERIALS CHEMISTRY AND PHYSICS
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2022
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IF 4.778
Jiao He,Congwei Li,Xinjian Cheng
Three chitosan-BODIPY probes were prepared in this work. The water solubility of original chitosan has been improved. Water soluble fluorescent probes were obtained. They also exhibited good sensing ability to Hg 2+ /Hg + ions. Firstly, through the amidation reaction, arginine, cysteine, and tryptophan were grafted respectively onto chitosan chains. And then chitosan-BODIPY probes were produced by means of Schiff base formation reaction. By this way, the high structural regularity of chitosan polymer chains was changed with introducing amino acids and fluorescent groups. It also endowed fluorescence sensing ability. They could recognize Hg 2+ /Hg + ions with the interaction of C N groups. It could selectively recognize Hg 2+ /Hg + in aqueous solution, the detection limits reached 0.747μM/0.783 μM. Moreover, by the introduction of hydrophilic groups, the contact angle of modified chitosan film was improved as well. It realized performance transformation from the hydrophobic to hydrophilic. The viscoelasticity , thermal, rheological properties and fluorescence properties of the hydrogels were investigated. C N groups not only acted as a binding site to coordinate with heavy metals, but also could enhance the water solubility of the fluorescent chitosan.
研究领域:
生物化学
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材料科学
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环境科学
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DOI
高影响因子
CARBOHYDRATE POLYMERS
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2016
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IF 4.219
Lishan Xu,Yaojie Zhang,Lizhi Wang
Dragon fruit is a tropical fruit with good taste. It can bring health benefits to human body. As one of the major bioactive components in this fruit, the polysaccharides might contribute to the health benefits. However, the precise structure information remains unknown. A leading polysaccharide of dragon fruit pulp, DFPP, was purified and identified by NMR and GC–MS. →4-β- d -Glc p A-1→, →6-β- d -Gal p -1→ and →4-α- l -Rha p -1→ constituted the backbone and α- l -Ara f -1 → 5-α- l -Ara f -1→ formed the branch chain. The precise structure was putatively identified as below. The molecular weight was 2.2 × 10 3 kDa. The structure information of polysaccharides will be helpful to understand this fruit. Download : Download high-res image (88KB) Download : Download full-size image
研究领域:
食品科学
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植物化学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
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2025
·
IF 4.7
Xian-Rui Zhang,Yong-Yan Su,Xiao-Han Zhang,Xi Liu,Lei Gao
This study focuses on significantly enhancing the water solubility of mefenamic acid (MFA) through an innovative pharmaceutical amine salt strategy. By analyzing the crystal structure of MFA single crystals, we found that the dimer structure formed through carboxylic acid O H⋯O hydrogen bonding between MFA molecules limits the exposure of its hydrophilic groups, which is a crucial factor contributing to its poor water solubility. To overcome this limitation, we meticulously synthesized three forms of MFA amine salts: MFA-DIP salt, MFA-DIPA salt, and MFA-HDA salt. Utilizing various technical approaches, including crystal structure analysis, Hirshfeld surface analysis, powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), infrared spectroscopy (IR), and fluorescence spectroscopy, we systematically investigated the structural characteristics and physicochemical properties of these amine salts. The results demonstrate that the hydrogen bonding interactions between MFA molecules are significantly enhanced upon salt formation, leading to favorable changes in the crystal structure and effective release of the previously restricted hydrophilic carboxylic acid groups, thereby significantly improving the water solubility of MFA. Notably, the solubility and dissolution rates of MFA-DIPA salt and MFA-HDA salt in water and pH 6.86 phosphate buffer solution were substantially increased. However, MFA-DIP salt exhibited salt decomposition during solubility testing, identified as a metastable crystalline form. This study not only provides practical strategies for improving the water solubility of MFA but also opens new perspectives for in-depth research on drug polymorphism stability and solubility optimization, offering potentially significant guidance for the field of pharmaceutical research and development.
研究领域:
药学
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材料科学
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产品关联
DOI
高影响因子
EUROPEAN POLYMER JOURNAL
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2021
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IF 4.598
Suyan He,Li Xiao,Luminita Marin,Yike Bai,Xinjian Cheng
The development of water-soluble polymer dyes is of great practical and scientific significance. In this article, small fluorescent molecule boron-dipyrromethene (BODIPY) bearing C=C bond was synthesized first. And then, via Suzuki reaction, recognition groups were introduced into the 2, 6 positions of BODIPY. Thus polymerizable fluorescent monomers were prepared. Finally, methacrylic acid (MAA) was copolymerized with the as-prepared small molecular fluorescent monomers via reversible addition-fragmentation chain transfer (RAFT) polymerization methodology. Four fully-water-soluble polymer sensors with BODIPY moieties in the end of the polymer chain were obtained eventually. In the presence of long PMAA chain, and by the assistance of it, BODIPY could be dissolved totally in water. These polymer sensors exhibited sensitive and selective recognition ability to Fe 3+ . Even the content rate of BODIPY was as low as 0.5% of the polymer (calculated from element analysis), the detection limit could reach 1.2 μM. The sensors with two recognition groups in one BODIPY unit were more sensitive than that with one recognition groups in each BODIPY unit. The sensing mechanism was investigated as well. By endowing the water solubility to organic sensors, the application scope could be greatly enlarged in sensing metal ions in aqueous environments. This work provides a method to develop water soluble high performance polymer sensors.
研究领域:
材料科学
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化学传感器
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分析化学
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产品关联
DOI
高影响因子
JOURNAL OF BIOMATERIALS SCIENCE-POLYMER EDITION
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2015
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IF 1.648
Ju Liang,Wenlan Wu,Danyu Lai,Junbo Li,Cailin Fang
A lipopeptide (LP)-containing KKGRGDS as the hydrophilic heads and lauric acid (C12) as the hydrophobic tails has been designed and prepared by standard solid-phase peptide synthesis technique. LP can self-assemble into spherical micelles with the size of ~30 nm in PBS (phosphate buffer saline) (pH 7.4). Curcumin-loaded LP micelles were prepared in order to increase the water solubility, sustain the releasing rate, and improve the tumor targeted delivery of curcumin. Water solubility, cytotoxicity, in vitro release behavior, and intracellular uptake of curcumin-loaded LP micelles were investigated. The results showed that LP micelles can increase the water solubility of curcumin 1.1 × 103 times and sustain the release of curcumin in a low rate. Curcumin-loaded LP micelles showed much higher cell inhibition than free curcumin on human cervix carcinoma (HeLa) and HepG2 cells. When incubating these curcumin-loaded micelles with HeLa and COS7 cells, due to the over-expression of integrins on cancer cells, the micelles can efficiently use the tumor-targeting function of RGD (functionalized peptide sequences: Arg-Gly-Asp) sequence to deliver the drug into HeLa cells, and better efficiency of the self-assembled LP micelles for curcumin delivery than crude curcumin was also confirmed by LCSM (laser confocal scanning microscope) assays. Combined with the enhanced solubility and higher cell inhibition, LP micelles reported in this study may be promising in clinical application for targeted curcumin delivery.
研究领域:
药剂学
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肿瘤学
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生物材料
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产品关联
DOI
PubMed
高影响因子
NEW JOURNAL OF CHEMISTRY
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2020
·Vol. 44
·期 14
·5218-5223
·
IF 3.288
Xiaona Hu,Ziruo Zhou,Lijun Han,Shujing Li,Wei Zhou
In recent years, phloretin has gained wide interest because of its antioxidant, antitumor, and skin whitening properties. However, its low water solubility and low stability make its usage in clinical application difficult, especially in water-based formulations. Phloretin–methyl-β-cyclodextrin (phloretin–Me-β-CD) and phloretin–(2-hydroxy)propyl-β-cyclodextrin (phloretin–HP-β-CD) inclusion complexes were prepared by the freeze-drying method. Phase solubility studies indicated that the ratio of the host–guest molecules was 1 : 1. The inclusion behavior has been investigated by X-ray diffraction (XRD), scanning electron microscopy (SEM), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), proton nuclear magnetic resonance (1H NMR), and two-dimensional rotational frame nuclear Overhauser effect spectroscopy (2D ROESY). The results showed that the water solubility of phloretin improved after encapsulation. The reducing power (RP) and 1,1-diphenyl-2-picryl-hydrazyl (DPPH) radical scavenging activity tests revealed that the antioxidant activity of phloretin improved after the formation of inclusion complexes with Me-β-CD and HP-β-CD. This could be a promising way to improve phloretin as a water-based formulation of antioxidants.
研究领域:
药剂学
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生物化学
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产品关联
DOI
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
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2019
·
IF 2.12
Xue-Pu Feng,Xin Na,Ya-Fei Guo,Rui Qian,Jian-Qiang Zhang,Zhen Chen,Rui Yang
1, 2-O, O-Diacetyllycorine (DALY) is one of the lycorine derivatives which has various biological properties. However, the bioavailability and clinical application of DALY was restrained because of its low water solubility and moderate antitumor activities . In order to improve its physicochemical properties, we prepared the inclusion complex of DALY with α-cyclodextrin (α-CD). The inclusion complex was characterized by UV, XRD, DSC , TG, 1 H, 2D NMR spectroscopy and its anticancer activity was evaluated in vitro against the human cell lines HCT116, A549, HepG2 and K562. The results demonstrated that DALY was encapsulated into the cavity of α-CD to form the complexes with 1:1 stoichiometry . The water solubility of DALY significantly increased for about 49 times after the inclusion complexation with α-CD. Furthermore, the cytotoxicity of DALY/α-CD against the examined cell lines was significantly increased for about 80 times compared to that of the free DALY. The improved physicochemical and biological properties of the inclusion complexes will be beneficial for its potential applications in the design and formulation of natural medicines.
研究领域:
药学
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肿瘤学
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天然药物化学
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产品关联
DOI
高影响因子
CHINESE JOURNAL OF POLYMER SCIENCE
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2019
·Vol. 38
·期 1
·9-16
·
IF 2.804
Man Shou-Kuo,Wang Xiao,Zheng Jin-Wen,An Ze-Sheng
Polymerization-induced self-assembly (PISA) is an efficient and versatile method to afford polymeric nano-objects with polymorphic morphologies. Compared to dispersion PISA syntheses based on soluble monomers, the vast majority of emulsion PISA formulations using insoluble monomers leads to kinetically-trapped spheres. Herein, we present aqueous emulsion PISA formulations generating worms and vesicles besides spheres. Two monomers with different butyl groups, n -butyl ( n BHMA) and tert -butyl ( t BHMA) α -hydroxymethyl acrylate, and thus possessing different water solubilities were synthesized via Baylis-Hillman reaction. Photoinitiated aqueous emulsion polymerizations of n BHMA and t BHMA employing poly(ethylene glycol) macromolecular chain transfer agents (macro-CTAs, PEG 45 -CTA, and PEG 113 -CTA) at 40 °C were systematically investigated to evaluate the effect of monomer structure and solubility on the morphology of the generated block copolymer nano-objects. Higher order morphologies including worms and vesicles were readily accessed for t BHMA, which has a higher water solubility than that of n BHMA. This study proves that plasticization of the core-forming block by water plays a key role in enhancing chain mobility required for morphological transition in emulsion PISA.
研究领域:
材料科学
·
化学
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产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）