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公开(公告)号：US20050129753A1
公开(公告)日：2005-06-16
申请号：US10988275
申请日：2004-11-12
IPC分类号： A61K9/127 , A61K31/704 , A61K31/404
CPC分类号： A61K9/127 , A61K31/704
摘要： A liposome composition having a protonatable therapeutic agent entrapped in the form of a salt with an glucuronate anion is disclosed. Methods for preparing the composition using an ammonium ion transmembrane gradient having glucuronate as the counterion are also disclsoed. In one embodiment where the protonatable agent is doxorubicin, the method of the invention has comparable loading efficiency, faster release rate, without compromising the therapeutic efficacy compared to loading with an ammonium ion gradient having sulfate as the counterion.
摘要翻译： 公开了一种具有以葡萄糖醛酸盐阴离子盐形式包埋的可质子治疗剂的脂质体组合物。 使用具有葡萄糖醛酸盐作为抗衡离子的铵离子跨膜梯度制备组合物的方法也被揭示。 在可质子化剂是多柔比星的一个实施方案中，与用硫酸盐作为抗衡离子的铵离子梯度负载相比，本发明的方法具有相当的加载效率，更快的释放速率，而不会降低治疗功效。
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2.发明申请公开(公告)号：US20080058294A1
公开(公告)日：2008-03-06
申请号：US11662172
申请日：2005-09-11
CPC分类号： A61K9/127 , A61K9/1271 , A61K31/573
摘要： The present invention provides pharmaceutical compositions comprising a glucocorticoid or glucocorticoid derivative stably encapsulated in a liposome. The glucocorticoid or glucocorticoid derivative is selected from an amphipathic weak base glucocorticoid or glucocorticoid derivative having a pKa equal or below 11 and a logD at pH 7 in the range between −2.5 and 1.5; or an amphipathic weak acid GC or GC derivative having a pKa above 3.5 and a logD at pH 7 in the range between −2.5 and 1.5. The therapeutic effect of the pharmaceutical composition of the invention was exhibited in vivo with appropriate models of multiple sclerosis and cancer.
摘要翻译： 本发明提供包含稳定包封在脂质体中的糖皮质激素或糖皮质激素衍生物的药物组合物。 糖皮质激素或糖皮质激素衍生物选自pKa等于或低于11的两亲性弱碱性糖皮质激素或糖皮质激素衍生物，在pH7的logD在-2.5和1.5之间的范围内; 或pKa高于3.5的两亲性弱酸GC或GC衍生物，pH7的logD在-2.5和1.5之间的范围内。 用适当的多发性硬化症和癌症模型在体内展示本发明的药物组合物的治疗效果。
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公开(公告)号：US4797285A
公开(公告)日：1989-01-10
申请号：US806084
申请日：1985-12-06
CPC分类号： A61K9/127 , A61K31/70 , Y10T428/2984
摘要： A drug/liposome composition comprising an aqueous suspension of liposomes and, entrapped in the lipid bilayer region of the liposomes, an anthraquinone drug containing quinone and hydroquinone functionalities on adjacent anthracene rings. An iron-specific trihydroxamic chelating agent contained in the bulk aqueous phase of the suspension and a lipophilic free-radical scavenger contained in the bilayer region of the liposome cooperate to reduce chemical modification of both drug and lipid components of the composition. A preferred composition containing doxorubicin and alpha-tocopherol entrapped in the liposomes, and ferrioxamine in the aqueous suspension phase is effective in treating human neoplasms, with significantly reduced side effects over those produced by free-drug administration.
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公开(公告)号：US4898735A
公开(公告)日：1990-02-06
申请号：US256844
申请日：1988-10-12
IPC分类号： A61K9/127
CPC分类号： A61K31/70 , A61K9/127 , Y10T428/2982
摘要： A drug/liposome composition comprising an aqueous suspension of liposomes and, entrapped in the lipid bilayer region of the liposomes, an anthraquinone drug containing quinone and hydroquinone functionalities on adjacent anthracene rings. An iron-specific trihydroxamic chelating agent contained in the bulk aqueous phase of the suspension and a lipophilic free-radical scavenger contained in the bilayer region of the liposome cooperate to reduce chemical modification of both drug and lipid components of the composition. A preferred composition containing doxorubicin and alpha-tocopherol entrapped in the liposomes, and ferrioxamine in the aqueous suspension phase is effective in treating human neoplasms, with significantly reduced side effects over those produced by free-drug administration.
摘要翻译： 一种药物/脂质体组合物，其包含脂质体的水性悬浮液，并且包埋在脂质体的脂质双层区域中，在相邻的蒽环上含有醌和氢醌官能团的蒽醌药物。 包含在悬浮液的本体水相中的铁特异性三羟肟酸螯合剂和包含在脂质体的双层区域中的亲脂性自由基清除剂配合以减少组合物的药物和脂质组分的化学修饰。 包含在脂质体中的多柔比星和α-生育酚的优选组合物和含水悬浮相中的铁草胺在治疗人类肿瘤方面是有效的，与通过游离药物给药产生的副作用相比显着降低。
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公开(公告)号：US5043166A
公开(公告)日：1991-08-27
申请号：US436469
申请日：1989-11-14
IPC分类号： A61K9/127
摘要： A drug/liposome composition comprising an aqueous suspension of liposomes and, entrapped in the lipid bilayer region of the liposomes, an anthraquinone drug containing quinone and hydroquinone functionalities on adjacent anthracene rings. An iron-specific trihydroxamic chelating agent contained in the bulk aqueous phase of the suspension and a lipophilic free-radical scavenger contained in the bilayer region of the liposome cooperate to reduce chemical modification of both drug and lipid components of the composition. A preferred composition containing doxorubicin and alpha-tocopherol entrapped in the liposomes, and ferrioxamine in the aqueous suspension phase is effective in treating human neoplasms, with significantly reduced side effects over those produced by free-drug administration.
摘要翻译： 一种药物/脂质体组合物，其包含脂质体的水性悬浮液，并且包埋在脂质体的脂质双层区域中，在相邻的蒽环上含有醌和氢醌官能团的蒽醌药物。 包含在悬浮液的本体水相中的铁特异性三羟肟酸螯合剂和包含在脂质体的双层区域中的亲脂性自由基清除剂配合以减少组合物的药物和脂质组分的化学修饰。 包含在脂质体中的多柔比星和α-生育酚的优选组合物和含水悬浮相中的铁草胺在治疗人类肿瘤方面是有效的，与通过游离药物给药产生的副作用相比显着降低。
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公开(公告)号：US10085940B2
公开(公告)日：2018-10-02
申请号：US14232332
申请日：2012-07-12
申请人： Alberto A. Gabizon , Yechezkel Barenholz , Hilary Shmeeda , John Maher , Ana Catarina Parente Pereira
发明人： Alberto A. Gabizon , Yechezkel Barenholz , Hilary Shmeeda , John Maher , Ana Catarina Parente Pereira
IPC分类号： A61K31/704 , A61K9/127 , A61K31/663 , A61K38/20 , A61K45/06 , A61K35/15 , A61K35/17 , A61K47/55 , A61K47/69 , A61K39/00
摘要： The present disclosure provides liposomes comprising a membrane and an intraliposomal aqueous water phase, the membrane comprising at least one liposome forming lipid and the intraliposomal aqueous water phase comprises a salt of a bisphosphonate together with an amphipathic weak base agent (PLAD). An example of a liposome is one comprising co encapsulated in the intraliposomal aqueous water phase N-containing bisphosphonate, such as alendronate, and an anthracycline such as doxorubicin which was shown to increase survival as compared to Doxil or to administrations of liposomal alendronate (PLA) and Doxil (separate liposomes). Such liposomes may carry a targeting moiety exposed at the liposome's outer surface, for example, conjugate of folic acid as a targeting moiety to folate receptor (FT-PLAD). Also provided by the present disclosure is a method of preparing the liposomes and methods of use of the liposomes, at times, in combination with additional active ingredients, such as γδ T-cells.
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公开(公告)号：US07985417B2
公开(公告)日：2011-07-26
申请号：US11246340
申请日：2005-10-07
IPC分类号： A61K9/127
CPC分类号： A61K9/1271 , A61K9/1277 , A61K47/6907 , A61K47/6913 , C07K16/32 , C07K2317/622
摘要： A method of inserting a lipid-linked moiety into a lipid assembly, such as a planar lipid monolayer or bilayer, a spherical lipid vesicle, a micelle, or an emulsion envelope monolayer is described. In the method, the lipid assembly and the lipid-linked moiety are contacted in the presence of microwave irradiation to permit the lipid-linked moiety to become associated with the lipid assembly. In one embodiment, the lipid assembly is a liposome and the lipid-linked moiety is a lipid-polymer. Compositions comprised of a lipid layer and of a lipid-linked moiety, prepared in accord with the method, are also described.
摘要翻译： 描述了将脂质连接的部分插入脂质组合物，例如平面脂质单层或双层，球形脂质囊泡，胶束或乳剂包膜单层中的方法。 在该方法中，脂质组装和脂质连接部分在微波照射的存在下接触以允许脂质连接部分与脂质组装相关联。 在一个实施方案中，脂质组合物是脂质体，脂质连接部分是脂质聚合物。 还描述了根据该方法制备的由脂质层和脂质连接部分组成的组合物。
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公开(公告)号：US20070087047A1
公开(公告)日：2007-04-19
申请号：US11633129
申请日：2006-12-01
CPC分类号： A61K9/0019 , A61K9/1271 , A61K31/00 , A61K38/12 , A61K38/1774 , A61K47/61 , A61K47/62 , A61K47/6911 , Y10S424/812 , A61K2300/00
摘要： A liposome composition comprising small, surface-bound effector molecules is disclosed. The liposomes have a surface layer of hydrophilic polymer chains, for enhanced circulation time in the bloodstream. The effector molecules are attached to the distal ends of the polymer chains. In one embodiment, the effector is polymyxin B, for treatment of septic shock.
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公开(公告)号：US20070082043A1
公开(公告)日：2007-04-12
申请号：US11492695
申请日：2006-07-25
CPC分类号： A61K9/127 , A61K38/09 , A61K38/2207 , A61K38/24 , A61K38/27 , A61K39/0005 , A61K2039/55555 , A61K2039/6031
摘要： The invention provides liposomal vehicles for encapsulating relatively high levels of water-soluble substances including immunogens directed against gastrin and gonadotropin releasing hormone. The liposome encapsulating large amounts of immunogens can be injected parentally to induce effective immune responses without exhibiting significant adverse tissue reactogenicity.
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公开(公告)号：US20050169979A1
公开(公告)日：2005-08-04
申请号：US11036690
申请日：2005-01-14
CPC分类号： A61K9/127 , A61K38/09 , A61K38/2207 , A61K38/27
摘要： The invention provides liposomal vehicles for encapsulating relatively high levels of immunogenic protein substances including immunogens directed against hormones and hormone receptors, such as gastrin and gonadotropin releasing hormone and their receptors. The liposome encapsulating large amounts of immunogens can be injected parenterally to induce effective immune responses without exhibiting significant adverse tissue reactogenicity. Methods for production of the liposomal vaccines and methods of their administration for treatment of diseases and conditions associated with the cognate hormones are also provided.
摘要翻译： 本发明提供用于包封相对高水平的免疫原性蛋白质物质的脂质体载体，包括针对激素和激素受体的免疫原，例如胃泌素和促性腺激素释放激素及其受体。 包封大量免疫原的脂质体可以肠胃外注射以诱导有效的免疫应答，而不显示显着的不利组织反应原性。 还提供了用于生产脂质体疫苗的方法及其用于治疗与同类激素相关的疾病和病症的施用方法。
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