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    Method and Compositions for Polymer Nanocarriers Containing Therapeutic Molecules
    6.
    发明申请
    Method and Compositions for Polymer Nanocarriers Containing Therapeutic Molecules 有权
    含有治疗分子的聚合物纳米载体的方法和组合物

    公开(公告)号：US20100316571A1

    公开(公告)日：2010-12-16

    申请号：US12739584

    申请日：2008-10-27

    申请人： Eric Simone ,  Vladimir R. Muzykantov ,  Thomas D. Dziubla

    发明人： Eric Simone ,  Vladimir R. Muzykantov ,  Thomas D. Dziubla

    IPC分类号： A61K49/00 ,  A61K38/00 ,  A61K9/14 ,  A61K38/43 ,  C12Q1/02

    CPC分类号： A61K9/5153 ,  A61K9/1075 ,  A61K47/60

    摘要： A method of controlling a physical characteristic of polymeric nanocarrier-encapsulated protein particles includes altering or selecting a weight percentage of a hydrophobic polymer block in a total amphiphilic diblock copolymer of a primary emulsion of a double emulsion, freeze-thaw technique. The primary emulsion is formed using a freeze-thaw cycle of the amphiphilic diblock copolymer and a protein having a molecular weight of up to or equal to 300,000 Da. Selection of the hydrophobic polymer block percentage alters one or more characteristics of the resulting nanoparticles, such as shape. Thus, as one aspect, a method of producing filamentous polymeric nanocarrier-encapsulated protein (i.e., active enzyme) particles involves forming a primary emulsion using a freeze-thaw cycle of (i) an amphiphilic diblock copolymer, which has a molecular weight of about 10,000 to about 100,000 Da and comprises a conjugate of the hydrophobic polymer block and a hydrophilic polymer block, wherein the amphiphilic diblock copolymer comprises greater than 81% to about 95% by weight of the hydrophobic polymer block; and a protein having a molecular weight of up to or equal to about 300,000 Da. Various compositions comprising such filamentous-shaped nanocarrier particles, and methods of use for diagnosis and therapy are disclosed.

    摘要翻译： 控制聚合物纳米载体包封的蛋白质颗粒的物理特性的方法包括改变或选择双乳液的初级乳液的全两亲双嵌段共聚物中的疏水性聚合物嵌段的重量百分数，冻融技术。 使用两亲二嵌段共聚物的冻融循环和分子量为至多300,000Da的蛋白质形成初级乳液。 疏水聚合物嵌段百分比的选择改变所得纳米颗粒的一种或多种特性，例如形状。 因此，一方面，生产丝状聚合物纳米载体包封的蛋白质（即活性酶）颗粒的方法包括使用（i）两亲性二嵌段共聚物（其分子量约为）的冷冻 - 解冻循环形成初级乳液 10,000至约100,000Da，并且包含疏水性聚合物嵌段和亲水性聚合物嵌段的共轭物，其中两亲性二嵌段共聚物包含大于疏水性聚合物嵌段重量的81％至约95％ 和分子量大于或等于约300,000Da的蛋白质。 公开了包含这种丝状纳米载体颗粒的各种组合物，以及用于诊断和治疗的方法。

    ANTIOXIDANT POLYMER NANOCARRIERS FOR USE IN PREVENTING OXIDATIVE INJURY
    7.
    发明申请
    ANTIOXIDANT POLYMER NANOCARRIERS FOR USE IN PREVENTING OXIDATIVE INJURY 有权
    用于预防氧化性损伤的抗氧化聚合物纳米颗粒

    公开(公告)号：US20090258078A1

    公开(公告)日：2009-10-15

    申请号：US12481876

    申请日：2009-06-10

    申请人： Vladimir R. Muzykantov ,  Thomas D. Dziubla

    发明人： Vladimir R. Muzykantov ,  Thomas D. Dziubla

    IPC分类号： A61K9/50 ,  A61P39/00

    CPC分类号： A61K38/44 ,  A61K9/5031 ,  A61K9/5153 ,  A61K9/5192 ,  A61K38/48 ,  A61K47/34

    摘要： The present invention is a method for encapsulating active protein in a polymeric nanocarrier. The instant method employs homogenization at subzero temperatures so that enzyme activity is retained. Enzymes which can be encapsulated by the present method include, for example, antioxidant enzymes and xenobiotic detoxifying enzymes. Encapsulation of an enzyme protects it from protease degradation and increases therapeutic half-life. Advantageously, polymeric nanoparticles of the invention are permeable to enzyme substrates and therefore enzymes encapsulated by the instant method can exert their effect without release from the nanocarrier. Methods for decomposing a reactive oxygen species, protecting against vascular oxidative stress, and detoxifying a xenobiotic are also provided.

    摘要翻译： 本发明是将活性蛋白质包封在聚合物纳米载体中的方法。 本方法在亚零温度下使用均匀化，从而保留酶活性。 可以通过本方法包封的酶包括例如抗氧化酶和异生物解毒酶。 酶的包封可以防止蛋白酶降解并增加治疗半衰期。 有利地，本发明的聚合物纳米颗粒对酶底物是可渗透的，因此通过本发明方法包封的酶可以发挥其作用而不从纳米载体释放。 还提供了分解活性氧物质，保护血管氧化应激和解毒异种生物的方法。

    METHOD AND COMPOSITIONS FOR POLYMER NANOCARRIERS CONTAINING THERAPEUTIC MOLECULES
    8.
    发明申请
    METHOD AND COMPOSITIONS FOR POLYMER NANOCARRIERS CONTAINING THERAPEUTIC MOLECULES 有权
    含有治疗分子的聚合物纳米颗粒的方法和组合物

    公开(公告)号：US20090110741A1

    公开(公告)日：2009-04-30

    申请号：US11925834

    申请日：2007-10-27

    申请人： Eric Simone ,  Vladimir R. Muzykantov ,  Thomas D. Dziubla

    发明人： Eric Simone ,  Vladimir R. Muzykantov ,  Thomas D. Dziubla

    IPC分类号： A61K9/16 ,  A61K9/50 ,  A61K38/00 ,  A61K38/54

    CPC分类号： A61K9/5153

    摘要： A method of controlling a physical characteristic of polymeric nanocarrier-encapsulated protein particles includes altering or selecting a weight percentage of a hydrophobic polymer block in a total amphiphilic diblock copolymer of a primary emulsion of a double emulsion, freeze-thaw technique. The primary emulsion is formed using a freeze-thaw cycle of the amphiphilic diblock copolymer and a protein having a molecular weight of up to or equal to 300,000 Da. Selection of the hydrophobic polymer block percentage alters one or more characteristics of the resulting nanoparticles, such as shape. Thus, as one aspect, a method of producing filamentous polymeric nanocarrier-encapsulated protein (i.e., active enzyme) particles involves forming a primary emulsion using a freeze-thaw cycle of (i) an amphiphilic diblock copolymer, which has a molecular weight of about 10,000 to about 100,000 Da and comprises a conjugate of the hydrophobic polymer block and a hydrophilic polymer block, wherein the amphiphilic diblock copolymer comprises greater than 81% to about 95% by weight of the hydrophobic polymer block; and a protein having a molecular weight of up to or equal to about 300,000 Da. Various compositions comprising such filamentous-shaped nanocarrier particles, and methods of use for diagnosis and therapy are disclosed.

    摘要翻译： 控制聚合物纳米载体包封的蛋白质颗粒的物理特性的方法包括改变或选择双乳液的初级乳液的全两亲双嵌段共聚物中的疏水性聚合物嵌段的重量百分数，冻融技术。 使用两亲二嵌段共聚物的冻融循环和分子量为至多300,000Da的蛋白质形成初级乳液。 疏水聚合物嵌段百分比的选择改变所得纳米颗粒的一种或多种特性，例如形状。 因此，一方面，生产丝状聚合物纳米载体包封的蛋白质（即活性酶）颗粒的方法包括使用（i）两亲性二嵌段共聚物（其分子量约为）的冷冻 - 解冻循环形成初级乳液 10,000至约100,000Da，并且包含疏水性聚合物嵌段和亲水性聚合物嵌段的共轭物，其中两亲性二嵌段共聚物包含大于疏水性聚合物嵌段重量的81％至约95％ 和分子量大于或等于约300,000Da的蛋白质。 公开了包含这种丝状纳米载体颗粒的各种组合物，以及用于诊断和治疗的方法。

    Method and compositions for polymer nanocarriers containing therapeutic molecules
    10.
    发明授权
    Method and compositions for polymer nanocarriers containing therapeutic molecules 有权
    含有治疗分子的聚合物纳米载体的方法和组合物

    公开(公告)号：US08568786B2

    公开(公告)日：2013-10-29

    申请号：US12739584

    申请日：2008-10-27

    申请人： Eric Simone ,  Vladimir R. Muzykantov ,  Thomas D. Dziubla

    发明人： Eric Simone ,  Vladimir R. Muzykantov ,  Thomas D. Dziubla

    IPC分类号： A61K49/00 ,  A61K38/00 ,  A61K9/14 ,  A61K38/43 ,  C12Q1/02

    CPC分类号： A61K9/5153 ,  A61K9/1075 ,  A61K47/60

    摘要： A method of controlling a physical characteristic of polymeric nanocarrier-encapsulated protein particles includes altering or selecting a weight percentage of a hydrophobic polymer block in a total amphiphilic diblock copolymer of a primary emulsion of a double emulsion, freeze-thaw technique. The primary emulsion is formed using a freeze-thaw cycle of the amphiphilic diblock copolymer and a protein having a molecular weight of up to or equal to 300,000 Da. Selection of the hydrophobic polymer block percentage alters one or more characteristics of the resulting nanoparticles, such as shape. Thus, as one aspect, a method of producing filamentous polymeric nanocarrier-encapsulated protein (i.e., active enzyme) particles involves forming a primary emulsion using a freeze-thaw cycle of (i) an amphiphilic diblock copolymer, which has a molecular weight of about 10,000 to about 100,000 Da and comprises a conjugate of the hydrophobic polymer block and a hydrophilic polymer block, wherein the amphiphilic diblock copolymer comprises greater than 81% to about 95% by weight of the hydrophobic polymer block; and a protein having a molecular weight of up to or equal to about 300,000 Da. Various compositions comprising such filamentous-shaped nanocarrier particles, and methods of use for diagnosis and therapy are disclosed.

    摘要翻译： 控制聚合物纳米载体包封的蛋白质颗粒的物理特性的方法包括改变或选择双乳液的初级乳液的全两亲双嵌段共聚物中的疏水性聚合物嵌段的重量百分数，冻融技术。 使用两亲二嵌段共聚物的冻融循环和分子量为至多300,000Da的蛋白形成初级乳液。 疏水聚合物嵌段百分比的选择改变所得纳米颗粒的一种或多种特性，例如形状。 因此，一方面，生产丝状聚合物纳米载体包封的蛋白质（即活性酶）颗粒的方法包括使用（i）两亲性二嵌段共聚物（其分子量约为）的冷冻 - 解冻循环形成初级乳液 10,000至约100,000Da，并且包含疏水性聚合物嵌段和亲水性聚合物嵌段的共轭物，其中两亲性二嵌段共聚物包含大于疏水性聚合物嵌段重量的81％至约95％ 和分子量大于或等于约300,000Da的蛋白质。 公开了包含这种丝状纳米载体颗粒的各种组合物，以及用于诊断和治疗的方法。