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Fuminori Ito - One of the best experts on this subject based on the ideXlab platform.

  • control of drug Loading Efficiency and drug release behavior in preparation of hydrophilic drug containing monodisperse plga microspheres
    Journal of Materials Science: Materials in Medicine, 2010
    Co-Authors: Fuminori Ito, Hiroyuki Fujimori, Hiroyuki Honnami, Hiroyoshi Kawakami, Kiyoshi Kanamura, Kimiko Makino
    Abstract:

    We prepared monodisperse poly(lactide-co-glycolide) (PLGA) microspheres containing blue dextran (BLD)--a hydrophilic drug--by membrane emulsification technique. The effects of electrolyte addition to the w(2) phase and significance of the droplet size ratio between primary (w(1)/o) and secondary (w(1)/o/w(2)) emulsions during the preparation of these microspheres was examined. The droplet size ratio was evaluated from the effect of stirring rate of the homogenizer when preparing the primary emulsion. The drug Loading Efficiency of BLD in these microspheres increased with stirring rate. It increased to approximately 90% when 2.0% NaCl was added to the w(2) phase. Drug release from these microspheres was slower than that when they were prepared without electrolyte addition. Despite the very high Efficiency drug release was gradual because BLD was distributed at the microspheres core. Relatively monodisperse hydrophilic-drug-containing PLGA microspheres with controlled drug Loading Efficiency and drug release behavior were prepared.

  • study of types and mixture ratio of organic solvent used to dissolve polymers for preparation of drug containing plga microspheres
    European Polymer Journal, 2009
    Co-Authors: Fuminori Ito, Hiroyuki Fujimori, Hiroyuki Honnami, Hiroyoshi Kawakami, Kiyoshi Kanamura, Kimiko Makino
    Abstract:

    The effects of the types and the ratios of various organic solvents used as a mixtures to dissolve poly (lactide-co-glycolide) (PLGA) by using a solvent evaporation method, a technique used to prepare polymer particles, were carefully studied in order to investigate their advantages in developing drug delivery system (DDS) formulations for the prepared microspheres. The particle size and drug Loading Efficiency of drug-containing PLGA microspheres were found to be dependent on the types of solvent used due to the interfacial tension between the organic solvent and water phase. The drug Loading Efficiency of monodisperse microspheres prepared by using a membrane emulsification technique employing organic solvents and high interfacial tension for dissolving the PLGA was increased in a controlled manner. The organic solvents with high interfacial tension in the water phase used for the preparation of polymer particles by means of the solvent evaporation method were found to be suitable in terms of improvement in the properties of DDS formulations.

  • Factors affecting the Loading Efficiency of water-soluble drugs in PLGA microspheres.
    Colloids and surfaces. B Biointerfaces, 2007
    Co-Authors: Fuminori Ito, Hiroyuki Fujimori, Kimiko Makino
    Abstract:

    Poly(lactide-co-glycolide), PLGA, microspheres containing blue dextran as a hydrophilic model drug were prepared by a solvent evaporation method from w/o/w emulsions using a micro homogenizer. Effects of surfactant concentration in oil phase, stirring time period and stirring rate in the preparation procedure of primary emulsion (w/o) upon drug-Loading Efficiency were evaluated. Stirring rate during preparation of primary emulsion and surfactant concentration in oil phase affected drug-Loading Efficiency and the particle size of primary emulsion. Microspheres having the higher drug-Loading Efficiency were obtained when size differences between the primary emulsions and the secondary ones were large. That is, when the diameter of the primary emulsion is much smaller than that of the secondary emulsion, PLGA microspheres with high-Loading Efficiency of blue dextran were obtained.

Kimiko Makino - One of the best experts on this subject based on the ideXlab platform.

  • control of drug Loading Efficiency and drug release behavior in preparation of hydrophilic drug containing monodisperse plga microspheres
    Journal of Materials Science: Materials in Medicine, 2010
    Co-Authors: Fuminori Ito, Hiroyuki Fujimori, Hiroyuki Honnami, Hiroyoshi Kawakami, Kiyoshi Kanamura, Kimiko Makino
    Abstract:

    We prepared monodisperse poly(lactide-co-glycolide) (PLGA) microspheres containing blue dextran (BLD)--a hydrophilic drug--by membrane emulsification technique. The effects of electrolyte addition to the w(2) phase and significance of the droplet size ratio between primary (w(1)/o) and secondary (w(1)/o/w(2)) emulsions during the preparation of these microspheres was examined. The droplet size ratio was evaluated from the effect of stirring rate of the homogenizer when preparing the primary emulsion. The drug Loading Efficiency of BLD in these microspheres increased with stirring rate. It increased to approximately 90% when 2.0% NaCl was added to the w(2) phase. Drug release from these microspheres was slower than that when they were prepared without electrolyte addition. Despite the very high Efficiency drug release was gradual because BLD was distributed at the microspheres core. Relatively monodisperse hydrophilic-drug-containing PLGA microspheres with controlled drug Loading Efficiency and drug release behavior were prepared.

  • study of types and mixture ratio of organic solvent used to dissolve polymers for preparation of drug containing plga microspheres
    European Polymer Journal, 2009
    Co-Authors: Fuminori Ito, Hiroyuki Fujimori, Hiroyuki Honnami, Hiroyoshi Kawakami, Kiyoshi Kanamura, Kimiko Makino
    Abstract:

    The effects of the types and the ratios of various organic solvents used as a mixtures to dissolve poly (lactide-co-glycolide) (PLGA) by using a solvent evaporation method, a technique used to prepare polymer particles, were carefully studied in order to investigate their advantages in developing drug delivery system (DDS) formulations for the prepared microspheres. The particle size and drug Loading Efficiency of drug-containing PLGA microspheres were found to be dependent on the types of solvent used due to the interfacial tension between the organic solvent and water phase. The drug Loading Efficiency of monodisperse microspheres prepared by using a membrane emulsification technique employing organic solvents and high interfacial tension for dissolving the PLGA was increased in a controlled manner. The organic solvents with high interfacial tension in the water phase used for the preparation of polymer particles by means of the solvent evaporation method were found to be suitable in terms of improvement in the properties of DDS formulations.

  • Factors affecting the Loading Efficiency of water-soluble drugs in PLGA microspheres.
    Colloids and surfaces. B Biointerfaces, 2007
    Co-Authors: Fuminori Ito, Hiroyuki Fujimori, Kimiko Makino
    Abstract:

    Poly(lactide-co-glycolide), PLGA, microspheres containing blue dextran as a hydrophilic model drug were prepared by a solvent evaporation method from w/o/w emulsions using a micro homogenizer. Effects of surfactant concentration in oil phase, stirring time period and stirring rate in the preparation procedure of primary emulsion (w/o) upon drug-Loading Efficiency were evaluated. Stirring rate during preparation of primary emulsion and surfactant concentration in oil phase affected drug-Loading Efficiency and the particle size of primary emulsion. Microspheres having the higher drug-Loading Efficiency were obtained when size differences between the primary emulsions and the secondary ones were large. That is, when the diameter of the primary emulsion is much smaller than that of the secondary emulsion, PLGA microspheres with high-Loading Efficiency of blue dextran were obtained.

Jianjun Cheng - One of the best experts on this subject based on the ideXlab platform.

  • high drug Loading and sub quantitative Loading Efficiency of polymeric micelles driven by donor receptor coordination interactions
    Journal of the American Chemical Society, 2018
    Co-Authors: Kaimin Cai, Jianjun Cheng, Min Lan, Xuesi Chen, Lichen Yin
    Abstract:

    Polymeric micelles are extensively used for the delivery of hydrophobic drugs, which, however, suffer from unsatisfactory drug Loading, colloidal uniformity, formulation stability, and drug release. Herein, we demonstrate a convenient strategy to prepare micelles with ultrahigh drug Loading via the incorporation of polymer–drug coordination interactions. An amphiphilic copolymer containing pendant phenylboronic acid as electron acceptor unit was synthesized, which afforded donor–acceptor coordination with doxorubicin to obtain micelles with ultrahigh drug Loading (∼50%), nearly quantitative Loading Efficiency (>95%), uniform size, and colloidal stability. Besides, the encapsulated drug can be effectively and selectively released in response to the high reactive oxygen species levels in cancer cells, which potentiated the anticancer efficacy and reduced systemic toxicity. Apart from doxorubicin, the current platform could be extended to other drugs with electron-donating groups (e.g., epirubicin and irinot...

  • dimeric drug polymeric nanoparticles with exceptionally high drug Loading and quantitative Loading Efficiency
    Journal of the American Chemical Society, 2015
    Co-Authors: Kaimin Cai, Ziyuan Song, Qian Yin, Yanfeng Zhang, Fatih M Uckun, Chen Jiang, Jianjun Cheng
    Abstract:

    Encapsulation of small-molecule drugs in hydrophobic polymers or amphiphilic copolymers has been extensively used for preparing polymeric nanoparticles (NPs). The Loadings and Loading efficiencies of a wide range of drugs in polymeric NPs, however, tend to be very low. In this Communication, we report a strategy to prepare polymeric NPs with exceptionally high drug Loading (>50%) and quantitative Loading Efficiency. Specifically, a dimeric drug conjugate bearing a trigger-responsive domain was designed and used as the core-constructing unit of the NPs. Upon co-precipitation of the dimeric drug and methoxypoly(ethylene glycol)-block-polylactide (mPEG-PLA), NPs with a dimeric drug core and a polymer shell were formed. The high-drug-Loading NPs showed excellent stability in physiological conditions. No premature drug or prodrug release was observed in PBS solution without triggering, while external triggering led to controlled release of drug in its authentic form.

Yin Xiao - One of the best experts on this subject based on the ideXlab platform.

  • Mesoporous bioactive glass scaffolds for efficient delivery of vascular endothelial growth factor
    Journal of Biomaterials Applications, 2012
    Co-Authors: Chengtie Wu, Jiang Chang, Yin Xiao
    Abstract:

    In this article, we, for the first time, investigated mesoporous bioactive glass scaffolds for the delivery of vascular endothelial growth factor. We have found that mesoporous bioactive glass scaffolds have significantly higher Loading Efficiency and more sustained release of vascular endothelial growth factor than non-mesoporous bioactive glass scaffolds. In addition, vascular endothelial growth factor delivery from mesoporous bioactive glass scaffolds has improved the viability of endothelial cells. The study has suggested that mesopore structures in mesoporous bioactive glass scaffolds play an important role in improving the Loading Efficiency, decreasing the burst release, and maintaining the bioactivity of vascular endothelial growth factor, indicating that mesoporous bioactive glass scaffolds are an excellent carrier of vascular endothelial growth factor for potential bone tissue engineering applications.

  • bioactive mesopore glass microspheres with controllable protein delivery properties by biomimetic surface modification
    Journal of Biomedical Materials Research Part A, 2010
    Co-Authors: Chengtie Wu, Yufeng Zhang, Xuebin Ke, Ross Crawford, Yin Xiao
    Abstract:

    Microsphere systems with the ideal properties for bone regeneration need to be bioactive, and at the same time possess the capacity for controlled protein/drug-delivery; however, the current crop of microsphere system fails to fulfill these properties. The aim of this study was to develop a novel protein-delivery system of bioactive mesoporous glass (MBG) microspheres by a biomimetic method through controlling the density of apatite on the surface of microspheres, for potential bone tissue regeneration. MBG microspheres were prepared by using the method of alginate cross-linking with Ca2+ ions. The cellular bioactivity of MBG microspheres was evaluated by investigating the proliferation and attachment of bone marrow stromal cell (BMSC). The Loading Efficiency and release kinetics of bovine serum albumin (BSA) on MBG microspheres were investigated after coprecipitating with biomimetic apatite in simulated body fluids (SBF). The results showed that MBG microspheres supported BMSC attachment and the Si containing ionic products from MBG microspheres stimulated BMSCs proliferation. The density of apatite on MBG microspheres increased with the length of soaking time in SBF. BSA-Loading Efficiency of MBG was significantly enhanced by co-precipitating with apatite. Furthermore, the Loading Efficiency and release kinetics of BSA could be controlled by controlling the density of apatite formed on MBG microspheres. Our results suggest that MBG microspheres are a promising protein-delivery system as a filling material for bone defect healing and regeneration.

Kaimin Cai - One of the best experts on this subject based on the ideXlab platform.

  • high drug Loading and sub quantitative Loading Efficiency of polymeric micelles driven by donor receptor coordination interactions
    Journal of the American Chemical Society, 2018
    Co-Authors: Kaimin Cai, Jianjun Cheng, Min Lan, Xuesi Chen, Lichen Yin
    Abstract:

    Polymeric micelles are extensively used for the delivery of hydrophobic drugs, which, however, suffer from unsatisfactory drug Loading, colloidal uniformity, formulation stability, and drug release. Herein, we demonstrate a convenient strategy to prepare micelles with ultrahigh drug Loading via the incorporation of polymer–drug coordination interactions. An amphiphilic copolymer containing pendant phenylboronic acid as electron acceptor unit was synthesized, which afforded donor–acceptor coordination with doxorubicin to obtain micelles with ultrahigh drug Loading (∼50%), nearly quantitative Loading Efficiency (>95%), uniform size, and colloidal stability. Besides, the encapsulated drug can be effectively and selectively released in response to the high reactive oxygen species levels in cancer cells, which potentiated the anticancer efficacy and reduced systemic toxicity. Apart from doxorubicin, the current platform could be extended to other drugs with electron-donating groups (e.g., epirubicin and irinot...

  • dimeric drug polymeric nanoparticles with exceptionally high drug Loading and quantitative Loading Efficiency
    Journal of the American Chemical Society, 2015
    Co-Authors: Kaimin Cai, Ziyuan Song, Qian Yin, Yanfeng Zhang, Fatih M Uckun, Chen Jiang, Jianjun Cheng
    Abstract:

    Encapsulation of small-molecule drugs in hydrophobic polymers or amphiphilic copolymers has been extensively used for preparing polymeric nanoparticles (NPs). The Loadings and Loading efficiencies of a wide range of drugs in polymeric NPs, however, tend to be very low. In this Communication, we report a strategy to prepare polymeric NPs with exceptionally high drug Loading (>50%) and quantitative Loading Efficiency. Specifically, a dimeric drug conjugate bearing a trigger-responsive domain was designed and used as the core-constructing unit of the NPs. Upon co-precipitation of the dimeric drug and methoxypoly(ethylene glycol)-block-polylactide (mPEG-PLA), NPs with a dimeric drug core and a polymer shell were formed. The high-drug-Loading NPs showed excellent stability in physiological conditions. No premature drug or prodrug release was observed in PBS solution without triggering, while external triggering led to controlled release of drug in its authentic form.