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    • 4. 发明授权
    • Amphoteric liposomes, a method of formulating an amphoteric liposome and a method of loading an amphoteric liposome
    • 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
    • US09283186B2
    • 2016-03-15
    • US13350137
    • 2012-01-13
    • Steffen PanznerSilke LutzEvgenios SiepiClaudia Müller
    • Steffen PanznerSilke LutzEvgenios SiepiClaudia Müller
    • C07D265/30A61K9/127
    • A61K9/127A61K9/1272A61K31/713Y02P20/582
    • 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.
    • 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。
    • 6. 发明申请
    • Amphoteric Liposomes, A Method Of Formulating An Amphoteric Liposome And A Method Of Loading An Amphoteric Liposome
    • 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
    • US20120135065A1
    • 2012-05-31
    • US13350137
    • 2012-01-13
    • Steffen PanznerSilke LutzEvgenios SiepiClaudia Müller
    • Steffen PanznerSilke LutzEvgenios SiepiClaudia Müller
    • A61K9/127A61K47/44A61K31/7088C07J43/00
    • A61K9/127A61K9/1272A61K31/713Y02P20/582
    • 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.
    • 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。