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    Amphoteric liposomes, a method of formulating an amphoteric liposome and a method of loading an amphoteric liposome
    1.
    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。

    Amphoteric Liposomes, A Method Of Formulating An Amphoteric Liposome And A Method Of Loading An Amphoteric Liposome
    3.
    发明申请
    Amphoteric Liposomes, A Method Of Formulating An Amphoteric Liposome And A Method Of Loading An Amphoteric Liposome 有权
    两性脂质体，制备两性脂质体的方法和加载两性脂质体的方法

    公开(公告)号：US20120135065A1

    公开(公告)日：2012-05-31

    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： A61K9/127 ,  A61K47/44 ,  A61K31/7088 ,  C07J43/00

    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。

    Lipids and lipid assemblies comprising transfection enhancer elements
    6.
    发明申请
    Lipids and lipid assemblies comprising transfection enhancer elements 有权
    包含转染增强子元件的脂质和脂质组件

    公开(公告)号：US20080306153A1

    公开(公告)日：2008-12-11

    申请号：US12004154

    申请日：2007-12-19

    申请人： Steffen Panzner ,  Evgenios Siepi ,  Silke Lutz ,  Christian Reinsch ,  Claudia Muller

    发明人： Steffen Panzner ,  Evgenios Siepi ,  Silke Lutz ,  Christian Reinsch ,  Claudia Muller

    IPC分类号： A61K31/20 ,  C07C53/122 ,  C07C231/00

    CPC分类号： A61K9/1272 ,  A61K9/127 ,  A61K31/7052 ,  A61K47/542 ,  A61K47/544 ,  A61K47/545 ,  A61K47/554 ,  A61K47/6911 ,  A61K48/0008 ,  A61K48/0025 ,  A61K48/0033 ,  A61K48/0041 ,  C07C229/24 ,  C12N15/88 ,  Y02P20/582

    摘要： Lipid assemblies, such as liposomes, comprising transfection enhancer elements (TEE's), which are complexed with the lipid assemblies by means of ionic interactions, or lipids incorporating such TEE's are disclosed for enhancing the fusogenicity of the lipid assemblies. The TEE's have the formula: hydrophobic moiety-pH sensitive hydrophilic moiety  (II) The pH sensitive hydrophilic moiety of each TEE is a weak acid having a pka of between 2 and 6 or a zwitterionic structure comprising a combination of acidic groups with weak bases having a pKa of between 3 and 8. Lipids incorporating one or more such TEEs have the formula (I): Lipid moiety-[Hydrophobic moiety-pH sensitive hydrophilic moiety]  (I)

    摘要翻译： 公开了脂质体组合物，例如脂质体，其包含通过离子相互作用与脂质组合物复合的转染增强子元件（TEE）或掺入这种TEE的脂质，用于增强脂质组件的融合性。 TEE具有以下公式：<？in-line-formula description =“In-line Formulas”end =“lead”？>疏水部分 - pH敏感亲水部分（II）<？in-line-formula description =“In- 线型“end =”tail“？>每个TEE的pH敏感的亲水部分是pka为2至6的弱酸或包含具有pKa在3和3之间的弱碱基的酸性基团的组合的两性离子结构 包含一个或多个这样的TEE的脂质具有式（I）：<？在线公式描述=“在线公式”end =“lead”？>脂质部分 - [疏水部分 - pH敏感亲水部分] （I）<？in-line-formula description =“In-line Formulas”end =“tail”？>