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    Novel amphiphilic copolymers and fabrication method thereof
    1.
    发明申请
    Novel amphiphilic copolymers and fabrication method thereof 审中-公开
    新型两亲性共聚物及其制造方法

    公开(公告)号：US20100203150A1

    公开(公告)日：2010-08-12

    申请号：US12320843

    申请日：2009-02-06

    申请人： Yu-Der Lee ,  Kuo-Yung Chang ,  Chia-Chun Lin

    发明人： Yu-Der Lee ,  Kuo-Yung Chang ,  Chia-Chun Lin

    IPC分类号： A61K9/14 ,  A61K31/7072

    CPC分类号： A61K9/1075 ,  A61K31/00

    摘要： The present invention discloses a comb-like amphiphilic copolymer comprising a hydrophilic segment and a hydrophobic segment. It also discloses a novel fabrication method for synthesizing said amphiphilic copolymers. A novel initiator comprising a drug molecule, e.g. 5′-DFUR, bonded to one or two macromolecules of a hydrophobic polymer is provided. A spherical micelle with core-shell structure is formed by self-aggregation of said amphiphilic copolymer. It discloses a micelle-like nanoparticle comprising one or more said amphiphilic copolymers. The nanoparticles contain said drug molecules innately with no need to encapsulate the desired drug into the nanoparticles. The nanoparticles can serve as micellar drug carriers for delivering the drug. A nanocarrier comprising said nanoparticle and an active water-insoluble substance, e.g. SN-38, Camptothecin, encapsulated in the nanoparticle is also disclosed. The nanocarriers can serve as a means of cocktail therapy to deliver a mixture of two kinds of drugs to affected parts.

    摘要翻译： 本发明公开了一种包含亲水链段和疏水片段的梳状两亲性共聚物。 它还公开了一种用于合成所述两亲性共聚物的新型制备方法。 包含药物分子的新型引发剂。 提供了与一个或两个大分子的疏水性聚合物键合的5'-DFUR。 通过所述两亲共聚物的自聚集形成具有核 - 壳结构的球形胶束。 它公开了包含一种或多种所述两亲性共聚物的胶束样纳米颗粒。 纳米颗粒本身含有所述药物分子，而不需要将所需药物包封到纳米颗粒中。 纳米颗粒可以用作用于递送药物的胶束药物载体。 包含所述纳米颗粒和活性水不溶性物质的纳米载体，例如。 还公开了包封在纳米颗粒中的喜树碱SN-38。 纳米载体可以作为鸡尾酒疗法的一种手段，将两种药物的混合物递送到受影响的部位。

    Drug-loaded poly (alkyl-cyanoacrylate) nanoparticles and process foe the preparation thereof
    2.
    发明申请
    Drug-loaded poly (alkyl-cyanoacrylate) nanoparticles and process foe the preparation thereof 有权
    药物负载聚（烷基 - 氰基丙烯酸酯）纳米颗粒及其制备方法

    公开(公告)号：US20080182776A1

    公开(公告)日：2008-07-31

    申请号：US11700226

    申请日：2007-01-31

    申请人： Yu-Der Lee ,  Chi-Yu Huang ,  Chih-Ming Chen

    发明人： Yu-Der Lee ,  Chi-Yu Huang ,  Chih-Ming Chen

    IPC分类号： A61K31/711 ,  A61K38/02 ,  A61K47/14 ,  A61K31/167 ,  A61K31/37

    CPC分类号： A61K9/5138 ,  A61K9/1075 ,  A61K9/5192 ,  A61K31/167 ,  A61K31/37 ,  A61K31/711

    摘要： A process for preparing the drug-loaded cyanoacrylate nanoparticles is described. The cyanoacrylate nanoparticles which effectively deliver biological and therapeutic agents are synthesized by miniemulsion polymerization with surfactant, pluronic F127 or F68. Before initiation of polymerization, active agents with particularly highly hydrophobicity are dissolved in cyanoacrylate monomer. Compared with the drug-loaded polyalkylcyanoacrylate nanoparticles produced by emulsion polymerization, those produced by miniemulsion polymerization possess higher loading and encapsulation efficiencies. While the content of dissolved agents increases, furthermore, the loading and encapsulation efficiencies increase concurrently.

    摘要翻译： 描述了制备负载药物的氰基丙烯酸酯纳米颗粒的方法。 通过与表面活性剂pluronic F127或F68的细乳液聚合合成有效递送生物和治疗剂的氰基丙烯酸酯纳米粒子。 在聚合开始之前，具有特别高度疏水性的活性剂溶解在氰基丙烯酸酯单体中。 与通过乳液聚合制备的载药聚氰基丙烯酸甲酯纳米颗粒相比，通过细乳液聚合制备的纳米颗粒具有更高的负载和包封效率。 而溶解剂的含量增加，此外，负载和封装效率同时增加。

    Drug-loaded poly (alkyl-cyanoacrylate) nanoparticles and process for the preparation thereof
    5.
    发明授权
    Drug-loaded poly (alkyl-cyanoacrylate) nanoparticles and process for the preparation thereof 有权
    载药聚（烷基 - 氰基丙烯酸酯）纳米颗粒及其制备方法

    公开(公告)号：US08679539B2

    公开(公告)日：2014-03-25

    申请号：US11700226

    申请日：2007-01-31

    申请人： Yu-Der Lee ,  Chi-Yu Huang ,  Chih-Ming Chen

    发明人： Yu-Der Lee ,  Chi-Yu Huang ,  Chih-Ming Chen

    IPC分类号： A61K9/14

    CPC分类号： A61K9/5138 ,  A61K9/1075 ,  A61K9/5192 ,  A61K31/167 ,  A61K31/37 ,  A61K31/711

    摘要： A process for preparing the drug-loaded cyanoacrylate nanoparticles is described. The cyanoacrylate nanoparticles which effectively deliver biological and therapeutic agents are synthesized by miniemulsion polymerization with surfactant, pluronic F127 or F68. Before initiation of polymerization, active agents with particularly highly hydrophobicity are dissolved in cyanoacrylate monomer. Compared with the drug-loaded polyalkylcyanoacrylate nanoparticles produced by emulsion polymerization, those produced by miniemulsion polymerization possess higher loading and encapsulation efficiencies. While the content of dissolved agents increases, furthermore, the loading and encapsulation efficiencies increase concurrently.

    摘要翻译： 描述了制备负载药物的氰基丙烯酸酯纳米颗粒的方法。 通过与表面活性剂pluronic F127或F68的细乳液聚合合成有效递送生物和治疗剂的氰基丙烯酸酯纳米粒子。 在聚合开始之前，具有特别高度疏水性的活性剂溶解在氰基丙烯酸酯单体中。 与通过乳液聚合制备的载药聚氰基丙烯酸甲酯纳米颗粒相比，通过细乳液聚合制备的纳米颗粒具有更高的负载和包封效率。 而溶解剂的含量增加，此外，负载和封装效率同时增加。

    Nanoparticles composed of alkyl-cyanoacrylate polymers
    6.
    发明申请
    Nanoparticles composed of alkyl-cyanoacrylate polymers 审中-公开
    由氰基丙烯酸烷基酯聚合物组成的纳米颗粒

    公开(公告)号：US20080138418A1

    公开(公告)日：2008-06-12

    申请号：US11634908

    申请日：2006-12-07

    申请人： Yu-Der Lee ,  Chi-Yu Huang

    发明人： Yu-Der Lee ,  Chi-Yu Huang

    IPC分类号： A61K9/14 ,  A61K47/14

    CPC分类号： A61K9/5138

    摘要： The role of nanoparticle composition as biodegradable carriers for variously therapeutical drugs is disclosed. Nanoparticles are synthesized by anion emulsion polymerization of two alkyl-cyanoacrylate monomers with adjusted content ratio. By modulating the compositions, particle size, hydrophobicity and degradation rate of the copolymers is controlled. Hence, to encapsulate wide range of therapeutical drugs, poly(alkyl cyanoacrylate) nanoparticles with feasible compositions are applied individually. The copolymer nanoparticles produced by n-butyl cyanoactylate (BCA) and 2-octyl cyanoacrylate (OCA), for example, were used therein. The nanoparticles composed of poly[(n-butyl cyanoacrylate)-co-(2-octyl cyanoacrylate)] and poly(2-octyl cyanoacrylate) might be adequate for therapeutical administration.

    摘要翻译： 公开了纳米颗粒组合物作为用于各种治疗药物的生物可降解载体的作用。 通过阴离子乳液聚合两种具有调节含量的氰基丙烯酸烷基酯单体合成纳米颗粒。 通过调节组合物，控制共聚物的粒度，疏水性和降解速率。 因此，为了封装广泛的治疗药物，单独使用具有可行组合物的聚（氰基丙烯酸烷基酯）纳米颗粒。 使用例如由氰基丙烯酸正丁酯（BCA）和2-辛基氰基丙烯酸酯（OCA）制备的共聚物纳米粒子。 由[（氰基丙烯酸正丁酯） - 共 - （2-辛基氰基丙烯酸酯）]和聚（2-辛基氰基丙烯酸酯）组成的纳米颗粒可能适合治疗。