NANOPARTICLE FORMULATIONS FOR DELIVERY OF NUCLEIC ACID COMPLEXES
    2.
    发明申请
    NANOPARTICLE FORMULATIONS FOR DELIVERY OF NUCLEIC ACID COMPLEXES 审中-公开
    用于递送核酸配合物的纳米颗粒配方

    公开(公告)号:WO2017075038A1

    公开(公告)日:2017-05-04

    申请号:PCT/US2016/058842

    申请日:2016-10-26

    Abstract: Aspects of the disclosure relate to particle formulations, e.g., nanoparticle formulations, methods of making particle formulations, and methods for delivery of oligonucleotides and/or synthetic RNA, e.g., for increasing gene expression in a targeted manner. In some embodiments, compositions and methods are provided that are useful for posttranscriptionally altering protein and/or RNA levels in a targeted manner. Aspects of the disclosure described herein provide compositions and methods that are useful for protecting RNAs from degradation (e.g., exonuclease mediated degradation).

    Abstract translation: 本公开的方面涉及颗粒制剂,例如纳米颗粒制剂,制备颗粒制剂的方法以及递送寡核苷酸和/或合成RNA的方法,例如用于以靶向方式增加基因表达 。 在一些实施方案中,提供了可用于以靶向方式转录后改变蛋白质和/或RNA水平的组合物和方法。 本文所述的公开内容的方面提供了可用于保护RNA免于降解(例如外切核酸酶介导的降解)的组合物和方法。

    PROCESS FOR THE PREPARATION OF DRUG LOADED MICROPARTICLES
    3.
    发明申请
    PROCESS FOR THE PREPARATION OF DRUG LOADED MICROPARTICLES 审中-公开
    制备药物加载微量元素的方法

    公开(公告)号:WO2016198113A1

    公开(公告)日:2016-12-15

    申请号:PCT/EP2015/063061

    申请日:2015-06-11

    Inventor: ALBAYRAK, Celal

    CPC classification number: A61K9/1647 A61K9/1694

    Abstract: Provided is a process for the production of nano- and/or microparticles containing a therapeutically active agent embedded in a polymer matrix or encapsulated by a polymer shell, and nano- and/or microparticles obtainable by the process, said process comprising the steps of: a) providing a solution of a polymer selected from polylactide, polyglycolide, and polyester copolymers comprising copolvmerized units of lactic acid and/or glycolic acid in an organic solvent SI having limited water solubility: b) providing a solution or dispersion of a therapeutically active agent in as solvent or mixture of organic solvents S2 comprising at least 50 vol.% benzyl alcohol, c) combining the solution or the solution and suspension provided in step a) and step b) to provide an organic phase which comprises dissolved polymer and dissolved therapeutically active agent in a mixture of the organic solvents S I and S2; d) agitating the organic phase provided in step c) in a vessel and adding an aqueous surfactant solution to the agitated organic phase in a volume ratio of at least 2: 1 in terms of the total volume of the aqueous surfactant solution to the total volume of the organic phase as provided in step c), thus causing the formation of a dispersion containing a continuous aqueous phase and a discontinuous organic phase; and e) allowing the spontaneous formation of the nano- and/or microparticles via transfer of organic solvent from the discontinuous organic phase into the continuous aqueous phase directly after the dispersion has been formed.

    Abstract translation: 本发明提供了一种制备包含嵌入聚合物基质中或由聚合物壳包封的治疗活性剂的纳米和/或微粒的方法,以及可通过该方法获得的纳米和/或微粒,所述方法包括以下步骤: a)提供选自聚丙交酯,聚乙交酯和包含乳酸和/或乙醇酸的共聚单体的聚酯共聚物的溶液在具有有限水溶性的有机溶剂SI中的溶液:b)提供治疗活性剂的溶液或分散体 作为包含至少50体积%苄醇的溶剂或有机溶剂S2的混合物,c)将溶液或溶液与步骤a)和步骤b)中提供的溶液和悬浮液混合以提供包含溶解的聚合物并在治疗上溶解的有机相 有机溶剂SI和S2的混合物中的活性剂; d)将容器中步骤c)中提供的有机相搅拌,并将表面活性剂水溶液以表面活性剂水溶液的总体积计至少为体积比为2:1的体积比添加到搅拌有机相中, 的步骤c)中提供的有机相,从而形成含有连续水相和不连续有机相的分散体; 以及e)通过有机溶剂在分散体形成之后直接将不连续有机相转移到连续水相中,允许自发形成纳米和/或微粒。

    OPHTHALMIC DRUG COMPOSITIONS
    6.
    发明申请
    OPHTHALMIC DRUG COMPOSITIONS 审中-公开
    眼药组合物

    公开(公告)号:WO2016042163A4

    公开(公告)日:2016-07-07

    申请号:PCT/EP2015071522

    申请日:2015-09-18

    Abstract: The present invention provides a composition for treatment of ophthalmic disease comprising a solid or semi-solid containing drug shaped as an elongated body for injection or delivery into tissue spaces of the eye. The composition may comprise a plurality of drug-containing particles and at least one excipient to form the drug particles into a flexible solid or a semisolid. The excipient comprises a substance that undergoes dissolution in the physiological conditions of the tissue space after injection to allow the microspheres to disperse and migrate in the tissue space. Formulations for the drug containing compositions, methods of fabrication and methods of use are also disclosed.

    Abstract translation: 本发明提供了用于治疗眼科疾病的组合物,其包含固体或半固体含有药物,其形状为用于注射或递送到眼睛组织空间中的细长体。 该组合物可以包含多种含药颗粒和至少一种赋形剂以将药物颗粒形成为柔性固体或半固体。 赋形剂包含在注射后在组织空间的生理条件下溶解的物质,以允许微球在组织空间中分散和迁移。 还公开了含有药物的组合物的制剂,制造方法和使用方法。

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