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    Amphoteric liposomes
    2.
    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
    3.
    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。

    Pharmaceutical compositions for local administration
    4.
    发明申请
    Pharmaceutical compositions for local administration 审中-公开
    用于局部给药的药物组合物

    公开(公告)号：US20060159737A1

    公开(公告)日：2006-07-20

    申请号：US11267423

    申请日：2005-11-04

    申请人： Steffen Panzner ,  Cornelia Panzner ,  Silke Lutz ,  Gerold Endert

    发明人： Steffen Panzner ,  Cornelia Panzner ,  Silke Lutz ,  Gerold Endert

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

    CPC分类号： A61K9/127 ,  A61K9/0031 ,  A61K9/1272 ,  A61K48/0025

    摘要： A pharmaceutical composition for local application is disclosed, said composition comprising a nucleic acid as a therapeutic agent, an excipient and a pharmaceutically acceptable vehicle therefor, said excipient comprising a liposome. The excipient comprises an amphoteric liposome having an isoelectric point between 4 and 7.4 and said composition is formulated to have a pH in the range 3 to 5. The composition may administered in the form of a colloidal suspension and may be buffered to the lower pH at the time of use by the addition of a suitable acidifying means to a substantially neutral suspension of the nucleic acid and excipient that may be more suitable for long-term storage of the composition. Alternatively, the composition may be lyophilised at the lower pH for subsequent reconstitution just prior to use with a suitable aqueous medium, such for example as substantially unbuffered water or saline.

    摘要翻译： 公开了用于局部应用的药物组合物，所述组合物包含作为治疗剂的核酸，赋形剂及其药学上可接受的载体，所述赋形剂包含脂质体。 赋形剂包含等电点在4和7.4之间的两性脂质体，所述组合物被配制成具有3至5范围内的pH。该组合物可以以胶态悬浮液的形式施用，并且可以缓冲至较低的pH值 通过将适当的酸化装置加入到可以更适合长期储存组合物的核酸和赋形剂的基本上中性的悬浮液上的使用时间。 或者，组合物可以在较低的pH下冻干，以便在使用之前用合适的水性介质，例如基本上无缓冲的水或盐水进行重组。

    Amphoteric liposomes, a method of formulating an amphoteric liposome and a method of loading an amphoteric liposome
    9.
    发明授权
    Amphoteric liposomes, a method of formulating an amphoteric liposome and a method of loading an amphoteric liposome 有权
    两性脂质体，配制两性脂质体的方法和加载两性脂质体的方法

    公开(公告)号：US09283186B2

    公开(公告)日：2016-03-15

    申请号：US13350137

    申请日：2012-01-13

    申请人： Steffen Panzner ,  Silke Lutz ,  Evgenios Siepi ,  Claudia Müller

    发明人： Steffen Panzner ,  Silke Lutz ,  Evgenios Siepi ,  Claudia Müller

    IPC分类号： C07D265/30 ,  A61K9/127

    CPC分类号： A61K9/127 ,  A61K9/1272 ,  A61K31/713 ,  Y02P20/582

    摘要： An amphoteric liposome composed of a mixture of lipids, said mixture comprising a cationic amphiphile, an anionic amphiphile and optionally one or more neutral amphiphiles, at least one of said cationic and anionic amphiphiles being chargeable and the respective amounts of said cationic and anionic amphiphiles being selected such there is a stoichiometric excess of positively charged cationic amphiphile at a first lower pH, a stoichiometric excess of negatively charged anionic amphiphile at a second higher pH and said mixture has an isoelectric point intermediate said first and second pHs; characterised in that said positively charged cationic and negatively charged anionic amphiphiles are adapted to form a lipid salt with one another at said isoelectric point. Also disclosed are methods of predicting the fusogenicity of an amphoteric liposome at a given pH, formulating an amphoteric liposome and loading an amphoteric liposome with a cargo moiety.

    摘要翻译： 由脂质混合物组成的两性脂质体，所述混合物包含阳离子两亲物，阴离子两亲物和任选的一个或多个中性两亲物，所述阳离子和阴离子两亲物中的至少一个是可带电的，并且相应量的所述阳离子和阴离子两亲物为 选择这样，在第二较低pH下，在第一较低pH下具有化学计量过量的带正电荷的阳离子两亲物，在第二较高pH下具有化学计量过量的带负电荷的阴离子两亲物，并且所述混合物具有介于所述第一和第二pH之间的等电点; 其特征在于所述带正电荷的阳离子和带负电荷的阴离子两亲物适于在所述等电点处彼此形成脂质盐。 还公开了在给定pH下预测两性脂质体的融合性的方法，配制两性脂质体并加载具有货物部分的两性脂质体。