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1.发明申请公开(公告)号：US20130149374A1
公开(公告)日：2013-06-13
申请号：US13697705
申请日：2010-11-12
IPC分类号： A61K9/127 , A61K31/713
CPC分类号： A61K9/1272 , A61K9/1271 , A61K9/1277 , A61K31/122 , A61K31/70 , A61K31/713
摘要： The present invention relates to asymmetric liposomes for high encapsulation efficiency of nucleic acids and hydrophilic anionic compounds, and to a method for preparing same, and specifically, to asymmetric liposomes consisting of a cationic lipid having a small head group as an internal lipid and a neutral or PEGylated lipid having a big head group as an external lipid, wherein nucleic acids and/or anionic compounds are encapsulated in the internal lipid. According to the present invention, asymmetric liposomes, in which nucleic acids and hydrophilic anionic compounds are encapsulated with high efficiency, may be prepared, and thus the same may be used for various purposes, such as gene therapy, and the delivery of hydrophilic anionic drugs which are difficult to prepare as prodrugs, and drug delivery, imaging, etc. can be carried out by encapsulating a fluorescent contrast agent in the liposome.
摘要翻译： 本发明涉及用于核酸和亲水性阴离子化合物的高包封效率的不对称脂质体及其制备方法，具体涉及由具有小头基团作为内部脂质和中性的阳离子脂质组成的不对称脂质体 或具有大头基的聚乙二醇化脂质作为外部脂质，其中核酸和/或阴离子化合物包封在内部脂质中。 根据本发明，可以制备其中核酸和亲水性阴离子化合物以高效率包封的不对称脂质体，因此可以用于各种目的，例如基因治疗和递送亲水性阴离子药物 其难以作为前药制备，并且药物递送，成像等可以通过将荧光对比剂包封在脂质体中来进行。
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2.发明授权公开(公告)号：US09326940B2
公开(公告)日：2016-05-03
申请号：US13697705
申请日：2010-11-12
IPC分类号： A61K9/127 , A61K31/122 , A61K31/70 , A61K31/713
CPC分类号： A61K9/1272 , A61K9/1271 , A61K9/1277 , A61K31/122 , A61K31/70 , A61K31/713
摘要： The present invention relates to asymmetric liposomes for high encapsulation efficiency of nucleic acids and hydrophilic anionic compounds, and to a method for preparing same, and specifically, to asymmetric liposomes consisting of a cationic lipid having a small head group as an internal lipid and a neutral or PEGylated lipid having a big head group as an external lipid, wherein nucleic acids and/or anionic compounds are encapsulated in the internal lipid. According to the present invention, asymmetric liposomes, in which nucleic acids and hydrophilic anionic compounds are encapsulated with high efficiency, may be prepared, and thus the same may be used for various purposes, such as gene therapy, and the delivery of hydrophilic anionic drugs which are difficult to prepare as prodrugs, and drug delivery, imaging, etc. can be carried out by encapsulating a fluorescent contrast agent in the liposome.
摘要翻译： 本发明涉及用于核酸和亲水性阴离子化合物的高包封效率的不对称脂质体及其制备方法，具体涉及由具有小头基团作为内部脂质和中性的阳离子脂质组成的不对称脂质体 或具有大头基的聚乙二醇化脂质作为外部脂质，其中核酸和/或阴离子化合物包封在内部脂质中。 根据本发明，可以制备其中核酸和亲水性阴离子化合物以高效率包封的不对称脂质体，因此可以用于各种目的，例如基因治疗和递送亲水性阴离子药物 其难以作为前药制备，并且药物递送，成像等可以通过将荧光对比剂包封在脂质体中来进行。
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