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  1. Article ; Online: Improving Solubility and Oral Bioavailability of Febuxostat by Polymer-Coated Nanomatrix.

    Yin, Yi-Fan / Guo, Yang / Song, Wen-Ding / Duan, Xiao-Chuan / Zheng, Xiu-Chai / Zhong, Ting / Zhang, Shuang / Yao, Xin / Xu, Mei-Qi / Zhang, Qiang / Zhang, Xuan

    AAPS PharmSciTech

    2018  Volume 19, Issue 2, Page(s) 934–940

    Abstract: Here, the mesoporous silica (Sylysia 350) was selected as mesoporous material, hydroxypropyl methylcellulose (HPMC) was selected as crystallization inhibitor, and febuxostat (FBT) was selected as model drug, respectively. The FBT-Sylysia-HPMC nanomatrix ( ...

    Abstract Here, the mesoporous silica (Sylysia 350) was selected as mesoporous material, hydroxypropyl methylcellulose (HPMC) was selected as crystallization inhibitor, and febuxostat (FBT) was selected as model drug, respectively. The FBT-Sylysia-HPMC nanomatrix (FBT@SHN) was prepared. The characteristics of FBT@SHN were investigated in vitro and in vivo. Our results indicated that the FBT in FBT@SHN was in amorphous form. The solubility and dissolution of FBT in FBT@SHN were significantly increased. The oral bioavailability of FBT in FBT@SHN was greatly improved 5.8-fold compared with that in FBT suspension. This nanomatrix could be used as a drug delivery platform for improving the oral bioavailability.
    MeSH term(s) Administration, Oral ; Animals ; Biological Availability ; Crystallization ; Drug Delivery Systems/methods ; Febuxostat/administration & dosage ; Febuxostat/chemistry ; Febuxostat/metabolism ; Gout Suppressants/administration & dosage ; Gout Suppressants/chemistry ; Gout Suppressants/metabolism ; Hypromellose Derivatives/administration & dosage ; Hypromellose Derivatives/chemistry ; Hypromellose Derivatives/metabolism ; Male ; Methylcellulose/chemistry ; Nanostructures/administration & dosage ; Nanostructures/chemistry ; Polymers/administration & dosage ; Polymers/chemistry ; Polymers/metabolism ; Rats ; Rats, Sprague-Dawley ; Silicon Dioxide/administration & dosage ; Silicon Dioxide/chemistry ; Silicon Dioxide/metabolism ; Solubility
    Chemical Substances Gout Suppressants ; Polymers ; Febuxostat (101V0R1N2E) ; Hypromellose Derivatives (3NXW29V3WO) ; Silicon Dioxide (7631-86-9) ; Methylcellulose (9004-67-5)
    Language English
    Publishing date 2018-02
    Publishing country United States
    Document type Journal Article
    ISSN 1530-9932
    ISSN (online) 1530-9932
    DOI 10.1208/s12249-017-0905-z
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Anti-tumour activity of low molecular weight heparin doxorubicin nanoparticles for histone H1 high-expressive prostate cancer PC-3M cells.

    Zhang, Shuang / Li, Zhan-Tao / Liu, Man / Wang, Jing-Ru / Xu, Mei-Qi / Li, Zhuo-Yue / Duan, Xiao-Chuan / Hao, Yan-Li / Zheng, Xiu-Chai / Li, Hui / Feng, Zhen-Han / Zhang, Xuan

    Journal of controlled release : official journal of the Controlled Release Society

    2018  Volume 295, Page(s) 102–117

    Abstract: Nucleus-targeting drug delivery systems (NTDDs) deliver chemotherapeutic agents to nuclei in order to improve the efficacy of anti-tumour therapy. Histone H1 (H1) plays a key role in establishing and maintaining higher order chromatin structures and ... ...

    Abstract Nucleus-targeting drug delivery systems (NTDDs) deliver chemotherapeutic agents to nuclei in order to improve the efficacy of anti-tumour therapy. Histone H1 (H1) plays a key role in establishing and maintaining higher order chromatin structures and could bind to cell membranes. In the present study, we selected H1 as a target to prepare a novel H1-mediated NTDD. Low molecular weight heparin (LMHP) and doxorubicin (DOX) were combined to form LMHP-DOX. Then, a novel NTDD consisting of LMHP-DOX nanoparticles (LMHP-DOX NPs) was prepared by self-assembly. The characteristics of LMHP-DOX and LMHP-DOX NPs were investigated. Histone H1 high-expressive prostate cancer PC-3M cell line was selected as the cell model. Cellular uptake, and the in vitro and in vivo anti-tumour activity of LMHP-DOX NPs were evaluated on H1 high-expressive human prostate cancer PC-3M cells. Our results indicated that intact LMHP-DOX NPs mediated by H1 could be absorbed by H1 high-expressive PC-3M cells, escape from the lysosomes to the cytoplasm, and localize in the perinuclear region via H1-mediated, whereby DOX could directly enter the cell nucleus and quickly increase the concentration of DOX in the nuclei of H1 high-expressive PC-3M cells to enhance the apoptotic activity of cancer cells. The anti-coagulant activity of LMHP-DOX NPs was almost completely diminished in rat blood compared with that of LMHP, indicating the safety of LMHP-DOX NPs. Compared to traditional NTDD strategies, LMHP-DOX NPs avoid the complicated modification of nucleus-targeting ligands and provide a compelling solution for the substantially enhanced nuclear uptake of chemotherapeutic agents for the development of more intelligent NTDDs.
    MeSH term(s) Animals ; Anticoagulants/administration & dosage ; Anticoagulants/pharmacokinetics ; Anticoagulants/pharmacology ; Antineoplastic Agents/administration & dosage ; Antineoplastic Agents/pharmacokinetics ; Antineoplastic Agents/pharmacology ; Cell Line, Tumor ; Doxorubicin/administration & dosage ; Doxorubicin/pharmacokinetics ; Doxorubicin/pharmacology ; Drug Delivery Systems ; Drug Liberation ; Heparin, Low-Molecular-Weight/administration & dosage ; Heparin, Low-Molecular-Weight/pharmacokinetics ; Heparin, Low-Molecular-Weight/pharmacology ; Histones/analysis ; Humans ; Male ; Nanoparticles/ultrastructure ; PC-3 Cells ; Prostatic Neoplasms/drug therapy ; Prostatic Neoplasms/pathology ; Rats, Sprague-Dawley
    Chemical Substances Anticoagulants ; Antineoplastic Agents ; Heparin, Low-Molecular-Weight ; Histones ; Doxorubicin (80168379AG)
    Language English
    Publishing date 2018-12-21
    Publishing country Netherlands
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 632533-6
    ISSN 1873-4995 ; 0168-3659
    ISSN (online) 1873-4995
    ISSN 0168-3659
    DOI 10.1016/j.jconrel.2018.12.034
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 2055: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)

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  3. Article ; Online: Effect of XlogP and Hansen Solubility Parameters on Small Molecule Modified Paclitaxel Anticancer Drug Conjugates Self-Assembled into Nanoparticles.

    Zhong, Ting / Hao, Yan-Li / Yao, Xin / Zhang, Shuang / Duan, Xiao-Chuan / Yin, Yi-Fan / Xu, Mei-Qi / Guo, Yang / Li, Zhan-Tao / Zheng, Xiu-Chai / Li, Hui / Zhang, Xuan

    Bioconjugate chemistry

    2018  Volume 29, Issue 2, Page(s) 437–444

    Abstract: Small molecule modified anticancer drug conjugates (SMMDCs) can self-assemble into nanoparticles (NPs) as therapeutic NP platforms for cancer treatment. Here we demonstrate that the XlogP and Hansen solubility parameters of paclitaxel (PTX) SMMDCs is ... ...

    Abstract Small molecule modified anticancer drug conjugates (SMMDCs) can self-assemble into nanoparticles (NPs) as therapeutic NP platforms for cancer treatment. Here we demonstrate that the XlogP and Hansen solubility parameters of paclitaxel (PTX) SMMDCs is essential for SMMDCs self-assembling into NPs. The amorphous state of PTX SMMDCs will also affect SMMDCs self-assembling into NPs. However, the antitumor activity of these PTX SMMDCs NPs decreased along with their XlogP values, indicating that a suitable XlogP value for designing the SMMDCs is important for self-assembling into NPs and for possessing antitumor activity. For higher level XlogP SMMDCs, a degradable linker should be considered in the design of SMMDCs to overcome the problem of lower antitumor activity. It is preferable that the hydrophilic groups in the SMMDCs should be present on the surface of self-assembling NPs.
    MeSH term(s) Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Breast Neoplasms/drug therapy ; Cell Survival/drug effects ; Humans ; Hydrophobic and Hydrophilic Interactions ; MCF-7 Cells ; Nanoparticles/chemistry ; Paclitaxel/analogs & derivatives ; Paclitaxel/pharmacology ; Small Molecule Libraries/chemistry ; Small Molecule Libraries/pharmacology ; Solubility
    Chemical Substances Antineoplastic Agents ; Small Molecule Libraries ; Paclitaxel (P88XT4IS4D)
    Language English
    Publishing date 2018-01-29
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1024041-x
    ISSN 1520-4812 ; 1043-1802
    ISSN (online) 1520-4812
    ISSN 1043-1802
    DOI 10.1021/acs.bioconjchem.7b00767
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 3400: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
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  4. Article ; Online: The theranostic efficiency of tumor-specific, pH-responsive, peptide-modified, liposome-containing paclitaxel and superparamagnetic iron oxide nanoparticles.

    Zheng, Xiu-Chai / Ren, Wei / Zhang, Shuang / Zhong, Ting / Duan, Xiao-Chuan / Yin, Yi-Fan / Xu, Mei-Qi / Hao, Yan-Li / Li, Zhan-Tao / Li, Hui / Liu, Man / Li, Zhuo-Yue / Zhang, Xuan

    International journal of nanomedicine

    2018  Volume 13, Page(s) 1495–1504

    Abstract: Background: In the present study, the tumor-specific, pH-responsive peptide H: Methods: The PTX/SPIO-SSL-H: Results: Our results of in vitro flow cytometry, in vivo imaging, and in vivo MR imaging confirmed the pH-responsive characteristic of H: ...

    Abstract Background: In the present study, the tumor-specific, pH-responsive peptide H
    Methods: The PTX/SPIO-SSL-H
    Results: Our results of in vitro flow cytometry, in vivo imaging, and in vivo MR imaging confirmed the pH-responsive characteristic of H
    Conclusion: Considering all our in vitro and in vivo results, we conclude that we developed targeting modified theranostic liposome which could achieve both role of antitumor and MRI.
    MeSH term(s) Animals ; Antineoplastic Agents/pharmacology ; Antineoplastic Agents/therapeutic use ; Cell Death/drug effects ; Cell Line, Tumor ; Drug Liberation ; Female ; Ferric Compounds/chemistry ; Flow Cytometry ; Humans ; Hydrogen-Ion Concentration ; Liposomes ; Magnetic Resonance Imaging ; Magnetite Nanoparticles/chemistry ; Mice, Inbred BALB C ; Mice, Nude ; Neoplasms/drug therapy ; Neoplasms/pathology ; Paclitaxel/pharmacology ; Paclitaxel/therapeutic use ; Peptides/chemistry ; Theranostic Nanomedicine/methods ; Tissue Distribution/drug effects
    Chemical Substances Antineoplastic Agents ; Ferric Compounds ; Liposomes ; Magnetite Nanoparticles ; Peptides ; ferric oxide (1K09F3G675) ; Paclitaxel (P88XT4IS4D)
    Language English
    Publishing date 2018-03-13
    Publishing country New Zealand
    Document type Journal Article
    ZDB-ID 2364941-0
    ISSN 1178-2013 ; 1176-9114
    ISSN (online) 1178-2013
    ISSN 1176-9114
    DOI 10.2147/IJN.S157082
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 6606: Show issues Location:
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  5. Article ; Online: Antitumor activity of the bioreductive prodrug 3-(2-nitrophenyl) propionic acid-paclitaxel nanoparticles (NPPA-PTX NPs) on MDA-MB-231 cells: in vitro and in vivo.

    Duan, Xiao-Chuan / Yao, Xin / Zhang, Shuang / Xu, Mei-Qi / Hao, Yan-Li / Li, Zhan-Tao / Zheng, Xiu-Chai / Liu, Man / Li, Zhuo-Yue / Li, Hui / Wang, Jing-Ru / Feng, Zhen-Han / Zhang, Xuan

    International journal of nanomedicine

    2018  Volume 14, Page(s) 195–204

    Abstract: Background: 3-(2-Nitrophenyl) propionic acid-paclitaxel (NPPA-PTX) is a paclitaxel (PTX) bioreductive prodrug synthesized by our lab. We hypothesize that NPPA-PTX can self-assemble to form nanoparticles (NPs).: Materials and methods: In the present ... ...

    Abstract Background: 3-(2-Nitrophenyl) propionic acid-paclitaxel (NPPA-PTX) is a paclitaxel (PTX) bioreductive prodrug synthesized by our lab. We hypothesize that NPPA-PTX can self-assemble to form nanoparticles (NPs).
    Materials and methods: In the present research, the theoretical partition coefficient (XlogP) and Hansen solubility parameters of NPPA-PTX were calculated. NPPA-PTX nanoparticles prepared by NPPA-PTX and DSPE-PEG (NPPA-PTX:DSPE-PEG =1:0.1, w/w) (NPPA-PTX@PEG NPs) were prepared and characterized. The cellular uptake, in vitro antitumor activity, in vivo targeting effect, tumor distribution, in vivo antitumor activity, and safety of NPPA-PTX@PEG NPs were investigated.
    Results: Our results indicate that NPPA-PTX can self-assemble to form NPPA-PTX@PEG NPs. Both the cellular uptake and safety of NPPA-PTX@PEG NPs were higher than those of Taxol. NPPA-PTX@PEG NPs could target tumor tissues by a passive targeting effect. In tumor tissues, NPPA-PTX@PEG NPs could completely transform into active PTX. The in vivo antitumor activity of NPPA-PTX@PEG NPs was confirmed in MDA-MB-231 tumor-bearing nude mice.
    Conclusion: The bioreductive prodrug NPPA-PTX could self-assemble to form NPs. The safety and antitumor activity of NPPA-PTX@PEG were confirmed in our in vitro and in vivo experiments. The NPPA-PTX@PEG NPs developed in this study could offer a new way of preparing bioreductive prodrug, self-assembled NPs suitable for antitumor therapy.
    MeSH term(s) Animals ; Apoptosis/drug effects ; Breast Neoplasms/drug therapy ; Breast Neoplasms/pathology ; Cell Proliferation/drug effects ; Female ; Humans ; In Vitro Techniques ; Mice ; Mice, Inbred BALB C ; Mice, Inbred ICR ; Mice, Nude ; Nanoparticles/administration & dosage ; Paclitaxel/administration & dosage ; Paclitaxel/analogs & derivatives ; Paclitaxel/pharmacology ; Phenylpropionates/administration & dosage ; Phenylpropionates/pharmacology ; Prodrugs/administration & dosage ; Prodrugs/pharmacology ; Tumor Cells, Cultured ; Xenograft Model Antitumor Assays
    Chemical Substances 3-(2-nitrophenyl)propionic acid-paclitaxel ; Phenylpropionates ; Prodrugs ; Paclitaxel (P88XT4IS4D)
    Language English
    Publishing date 2018-12-24
    Publishing country New Zealand
    Document type Journal Article
    ZDB-ID 2364941-0
    ISSN 1178-2013 ; 1176-9114
    ISSN (online) 1178-2013
    ISSN 1176-9114
    DOI 10.2147/IJN.S186556
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 6606: Show issues Location:
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