INJECTABLE PASTES BASED ON OPPOSITELY CHARGED POLYMER/CALCIUM PHOSPHATE HYBRID NANOPARTICLES
    3.
    发明申请
    INJECTABLE PASTES BASED ON OPPOSITELY CHARGED POLYMER/CALCIUM PHOSPHATE HYBRID NANOPARTICLES 审中-公开
    基于对电荷聚合物/磷酸钙混合纳米粒子的可注射糊剂

    公开(公告)号:WO2017209823A2

    公开(公告)日:2017-12-07

    申请号:PCT/US2017/022198

    申请日:2017-03-13

    IPC分类号: A61K9/51

    摘要: Provided herein are polymer-stabilized CaP nanoparticle formulations and related methods of manufacture. In certain embodiments, the methods reliably and selectively form nanoparticles with homogenous size, charge, and morphology. The CaP nanoparticles include calcium ions and phosphate ions with an ionic polymer, thereby forming stable hybrid nanoparticles. The CaP nanoparticle formulations include powders, suspensions and injectable pastes. According to various embodiments, the polymer-stabilized CaP nanoparticles may be polycation-stabilized (CaP/polymer(+) nanoparticles) or polyanion-stabilized (CaP/polymer(-) nanoparticles). The CaP/polymer nanoparticles can be freeze-dried and stored for months with no loss of properties or changes to their morphology.

    摘要翻译: 本文提供了聚合物稳定的CaP纳米颗粒制剂和相关的制造方法。 在某些实施方案中,所述方法可靠且选择性地形成具有均匀尺寸,电荷和形态的纳米颗粒。 CaP纳米粒子包括钙离子和磷酸根离子与离子聚合物,从而形成稳定的混合纳米粒子。 CaP纳米粒子制剂包括粉剂,混悬剂和可注射糊剂。 根据各种实施例,聚合物稳定的CaP纳米粒子可以是聚阳离子稳定的(CaP /聚合物(+)纳米粒子)或聚阴离子稳定的(CaP /聚合物( - )纳米粒子)。 可以将CaP /聚合物纳米颗粒冷冻干燥并储存数月,而不损失性质或改变其形态。

    CORE-SHELL PARTICLES
    4.
    发明申请
    CORE-SHELL PARTICLES 审中-公开
    核壳颗粒

    公开(公告)号:WO2017184085A1

    公开(公告)日:2017-10-26

    申请号:PCT/SG2017/050226

    申请日:2017-04-21

    发明人: YONG, Gen LIU, Ye

    IPC分类号: A61K9/51 A61K9/54

    CPC分类号: A61K9/5115

    摘要: There is provided a core-shell particle comprising a core comprising at least one active agent and a method of forming said core-shell particle, wherein said core having ions of an additive surrounding a surface of said core; and an encapsulating shell comprising (i) a polymer and/or (ii) a metal or a semi-metal oxide, phosphate or carbonate. In a preferred embodiment, chondroitin sulphate nanocrystals is first prepared by using pH recrystallization method. Sodium citrate is then added to form citrate ions-capped chondroitin sulphate particles. Poly L-lysine (PLL) and tetramethoxysilane (TMOS) are subsequently added to form a silica shell surrounding the citrate-ions capped chondroitin sulphate particles, and thus forming the claimed core-shell particle. The particles may be used as sustained release formulations in therapy.

    摘要翻译: 提供了包含含有至少一种活性剂的核的核 - 壳颗粒和形成所述核 - 壳颗粒的方法,其中所述核具有围绕所述核的表面的添加剂的离子 ; 和包含(i)聚合物和/或(ii)金属或半金属氧化物,磷酸盐或碳酸盐的包封壳。 在一个优选的实施方案中,首先通过使用pH重结晶方法制备硫酸软骨素纳米晶体。 然后加入柠檬酸钠以形成柠檬酸根离子封端的硫酸软骨素颗粒。 随后加入聚L-赖氨酸(PLL)和四甲氧基硅烷(TMOS)以形成围绕柠檬酸盐离子封端的硫酸软骨素颗粒的二氧化硅壳,并因此形成要求保护的核 - 壳颗粒。 这些颗粒可以在治疗中用作缓释制剂。

    COMPOUNDS AND COMPOSITIONS FOR TARGETING BRAIN INJURIES AND METHODS OF USE THEREOF
    7.
    发明申请
    COMPOUNDS AND COMPOSITIONS FOR TARGETING BRAIN INJURIES AND METHODS OF USE THEREOF 审中-公开
    用于预防脑损伤的化合物和组合物及其使用方法

    公开(公告)号:WO2017040976A1

    公开(公告)日:2017-03-09

    申请号:PCT/US2016/050168

    申请日:2016-09-02

    IPC分类号: C07K5/103 A61K9/00

    摘要: Disclosed are methods and compositions for selectively targeting sites of traumatic brain injury (TBI). A brain injury-specific 4-amino acid peptide (sequence CAQK), identified by in vivo phage display screening in mice with acute brain injury, shows selective binding to mouse and human brain injury lesions, and when systemically injected, specifically homes to sites of injury in penetrating and non-penetrating (controlled cortical impact) brain injury models. Also disclosed are methods and compositions for delivering therapeutic compounds to such sites. CAQK-coated nanoparticles containing silencing oligonucleotides provide an alternative to local delivery of therapeutics, which is invasive and can add complications to the injury.

    摘要翻译: 公开了用于选择性靶向创伤性脑损伤(TBI)部位的方法和组合物。 通过在具有急性脑损伤的小鼠中的体内噬菌体展示筛选鉴定的脑损伤特异性4-氨基酸肽(序列CAQK)显示出与小鼠和人类脑损伤病变的选择性结合,并且当全身注射时, 穿透性和非穿透性(受控皮质冲击)脑损伤模型的损伤。 还公开了将治疗化合物递送到这些部位的方法和组合物。 含有沉默寡核苷酸的CAQK包被的纳米颗粒提供局部递送治疗剂的替代方法,其是侵入性的并且可以增加损伤的并发症。

    NEGATIVELY CHARGED SELF-ASSEMBLING SUPPORTED LIPID BILAYER ON MESOPOROUS SILICA NANOPARTICLES, METHOD OF SYNTHESIS AND USE AS A NANOVECTOR
    9.
    发明申请
    NEGATIVELY CHARGED SELF-ASSEMBLING SUPPORTED LIPID BILAYER ON MESOPOROUS SILICA NANOPARTICLES, METHOD OF SYNTHESIS AND USE AS A NANOVECTOR 审中-公开
    在多孔二氧化硅纳米粒子上自负荷自组装支持的双面胶体,合成方法和用作纳米线

    公开(公告)号:WO2017013250A1

    公开(公告)日:2017-01-26

    申请号:PCT/EP2016/067546

    申请日:2016-07-22

    IPC分类号: A61K9/127 A61K9/51

    摘要: The invention is directed to a method for manufacturing a negatively charged supported lipid bilayer. Said method comprises the steps of preparing a formulation comprising at least three lipids (1,2-dioleoyl-sn-glycero-3-phospho-L- serine (DOPS), cholesterol and at least one lipid different from DOPS and cholesterol) dissolved in a first solvent, of evaporating said first solvent, of adding an aqueous formulation of mesoporous silica nanoparticles, of performing an ultra- sonication and of performing a centrifugation. Said method is remarkable in that the number of equivalents of cholesterol relative to one equivalent of DOPS is comprised between 2.30 and 2.70. The invention is further directed to negatively charged supported lipid bilayer on a mesoporous silica nanoparticle comprising cholesterol, 1,2-dioleoyl-sn-glycero-3-phospho-L-serine (DOPS) and at least one lipid different from DOPS and cholesterol.

    摘要翻译: 本发明涉及制造带负电荷的脂质双层的方法。 所述方法包括以下步骤:制备包含至少三种脂质(1,2-二油酰-sn-甘油-3-磷酸-L-丝氨酸(DOPS)),胆固醇和至少一种不同于DOPS和胆固醇的脂质) 蒸发所述第一溶剂的第一溶剂,加入介孔二氧化硅纳米颗粒的水性制剂,进行超声处理和进行离心。 所述方法是显着的,因为胆固醇相对于1当量的DOPS的当量数在2.30和2.70之间。 本发明进一步涉及包含胆固醇,1,2-二油酰-sn-甘油-3-磷酸-L-丝氨酸(DOPS)和至少一种不同于DOPS和胆固醇的脂质的介孔二氧化硅纳米颗粒上带负电荷的支持脂质双层。

    INORGANIC CONTROLLED RELEASE PARTICLES WITH FAST DRUG LOADING
    10.
    发明申请
    INORGANIC CONTROLLED RELEASE PARTICLES WITH FAST DRUG LOADING 审中-公开
    无机控制释放颗粒与快速药物装载

    公开(公告)号:WO2016204896A1

    公开(公告)日:2016-12-22

    申请号:PCT/US2016/032408

    申请日:2016-05-13

    IPC分类号: A61K9/14 A61K9/50

    CPC分类号: A61K9/5115 A61K9/0019

    摘要: Disclosed herein are nanoparticles comprising an inorganic material having pores that can quickly absorb pharmaceutical moieties and then release such moieites in a controlled fashion for an extended period of time. The nanoparticles can be aggregated in order to form microaggregates that provide the same advantages of quick absorption and controlled release of pharmaceutical moieties. Quick absorption permits the preparation of drug-loaded nanoparticles and microaggregates essentially contemporaneously with the time of treatment, such as during a surgical process. Methods of preparing such nanoparticles and microaggregates are also provided, as are methods for administering a pharmaceutical moiety using the nanoparticles and microaggregates.

    摘要翻译: 本文公开了包含具有孔的无机材料的纳米颗粒,其可以快速吸收药物部分,然后以受控的方式长时间地释放这样的粘粒。 可以聚集纳米颗粒以形成提供药物部分的快速吸收和受控释放的相同优点的微团聚体。 快速吸收允许在治疗时间基本同时制备负载药物的纳米颗粒和微团聚体,例如在外科手术过程中。 还提供了制备这种纳米颗粒和微团聚体的方法,以及使用纳米颗粒和微团聚体施用药物部分的方法。