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    Amphoteric liposomes
    4.
    发明授权
    Amphoteric liposomes 有权
    两性脂质体

    公开(公告)号：US09066867B2

    公开(公告)日：2015-06-30

    申请号：US12807707

    申请日：2010-09-09

    申请人： Steffen Panzner ,  Yvonne Kerwitz ,  Una Rauchhaus ,  Silke Lutz ,  Gerold Endert

    发明人： Steffen Panzner ,  Yvonne Kerwitz ,  Una Rauchhaus ,  Silke Lutz ,  Gerold Endert

    IPC分类号： A61K48/00 ,  A61K9/127 ,  A61K9/00 ,  C12N15/88

    CPC分类号： A61K9/1271 ,  A61K9/0019 ,  A61K9/127 ,  A61K9/1272 ,  A61K31/713 ,  A61K48/00 ,  C12N15/1138 ,  C12N15/88 ,  C12N2310/11 ,  C12N2320/32

    摘要： A serum-stable mixture of lipids capable of encapsulating an active agent to form a liposome, said mixture comprising phosphatidylcholine and phosphatidylethanolamine in a ratio in the range of about 0.5 to about 8. The mixture may also include pH sensitive anionic and cationic amphiphiles, such that the mixture is amphoteric, being negatively charged or neutral at pH 7.4 and positively charged at pH 4. Amphoteric liposomes comprising such a mixture may be used for encapsulating nucleic acid therapeutics, such as oligonucleotides and DNA plasmids. The drug/lipid ratio may be adjusted to target the liposomes to particular organs or other sites in the body.

    摘要翻译： 能够包封活性剂形成脂质体的脂质的血清稳定混合物，所述混合物包含比例在约0.5至约8范围内的磷脂酰胆碱和磷脂酰乙醇胺。该混合物还可包括pH敏感的阴离子和阳离子两亲物， 混合物是两性的，在pH7.4下带负电荷或中性，并在pH4下带正电。包含这种混合物的两性脂质体可用于包封核酸治疗剂，例如寡核苷酸和DNA质粒。 可以调节药物/脂质比以将脂质体靶向体内特定器官或其他部位。

    Amphoteric liposomes
    5.
    发明申请
    Amphoteric liposomes 审中-公开
    两性脂质体

    公开(公告)号：US20070104775A1

    公开(公告)日：2007-05-10

    申请号：US11521857

    申请日：2006-09-15

    申请人： Steffen Panzner ,  Yvonne Kerwitz ,  Una Rauchhaus ,  Silke Lutz ,  Gerold Endert

    发明人： Steffen Panzner ,  Yvonne Kerwitz ,  Una Rauchhaus ,  Silke Lutz ,  Gerold Endert

    IPC分类号： A61K48/00 ,  A61K9/127 ,  C12N15/88

    CPC分类号： A61K9/1271 ,  A61K9/0019 ,  A61K9/127 ,  A61K9/1272 ,  A61K31/713 ,  A61K48/00 ,  C12N15/1138 ,  C12N15/88 ,  C12N2310/11 ,  C12N2320/32

    摘要： A serum-stable mixture of lipids capable of encapsulating an active agent to form a liposome, said mixture comprising phosphatidylcholine and phosphatidylethanolamine in a ratio in the range of about 0.5 to about 8. The mixture may also include pH sensitive anionic and cationic amphiphiles, such that the mixture is amphoteric, being negatively charged or neutral at pH 7.4 and positively charged at pH 4. Amphoteric liposomes comprising such a mixture may be used for encapsulating nucleic acid therapeutics, such as oligonucleotides and DNA plasmids. The drug/lipid ratio may be adjusted to target the liposomes to particular organs or other sites in the body.

    摘要翻译： 能够包封活性剂形成脂质体的脂质的血清稳定混合物，所述混合物包含比例在约0.5至约8范围内的磷脂酰胆碱和磷脂酰乙醇胺。该混合物还可包括pH敏感的阴离子和阳离子两亲物， 混合物是两性的，在pH7.4下带负电荷或中性，并在pH4下带正电。包含这种混合物的两性脂质体可用于包封核酸治疗剂，例如寡核苷酸和DNA质粒。 可以调节药物/脂质比以将脂质体靶向体内特定器官或其他部位。

    Efficient Method For Loading Amphoteric Liposomes With Nucleic Acid Active Substances
    6.
    发明申请
    Efficient Method For Loading Amphoteric Liposomes With Nucleic Acid Active Substances 审中-公开
    用核酸活性物质加载两性脂质体的有效方法

    公开(公告)号：US20120021042A1

    公开(公告)日：2012-01-26

    申请号：US12225030

    申请日：2007-03-16

    申请人： Steffen Panzner ,  Gerold Endert ,  Una Rauchhaus ,  Natalie Herzog ,  Claudia Muller

    发明人： Steffen Panzner ,  Gerold Endert ,  Una Rauchhaus ,  Natalie Herzog ,  Claudia Muller

    IPC分类号： A61K9/127 ,  A61K31/713 ,  A61K38/02 ,  A61K48/00 ,  C12N5/00

    CPC分类号： A61K9/1277 ,  A61K9/127 ,  A61K31/7088 ,  C12N15/88

    摘要： A method for preparing amphoteric liposomes loaded with polyanionic active agent as cargo, characterised by admixing an aqueous solution of said polyanionic active agent and an alcoholic solution of one or more amphiphiles and buffering said admixture to an acidic pH, said one or more amphiphiles being susceptible of forming amphoteric liposomes at said acidic pH, thereby to form such amphoteric liposomes in suspension encapsulating said active agent under conditions such that said liposomes form aggregates, and thereafter treating said suspension to dissociate said aggregates. Also disclosed are nucleic acid loaded amphoteric liposomes produced in accordance with the method, wherein said nucleic acids are oligonucleotides and said liposomes are multilamellar.

    摘要翻译： 一种制备负载聚阴离子活性剂作为货物的两性脂质体的方法，其特征在于将所述聚阴离子活性剂的水溶液与一种或多种两亲物的醇溶液混合并将所述混合物缓冲至酸性pH，所述一种或多种两亲物易感 在所述酸性pH下形成两性脂质体，从而在使所述脂质体形成聚集体的条件下形成包封所述活性剂的悬浮液的这种两性脂质体，然后处理所述悬浮液以离解所述聚集体。 还公开了根据该方法生产的核酸负载的两性脂质体，其中所述核酸是寡核苷酸，所述脂质体是多层的。