申请人:Panzner Steffen
公开号:US20080306153A1
公开(公告)日:2008-12-11
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)
本发明揭示了包含转染增强元素(TEE)的脂质组装体,例如脂质体,这些TEE通过离子相互作用与脂质组装体形成复合物,或者包含此类TEE的脂质。这些TEE的公式为:疏水基团-pH敏感亲水基团(II)。每个TEE的pH敏感亲水基团是一种弱酸,其pka在2到6之间,或者是包含酸性基团和pKa在3到8之间的弱碱性基团的双电离结构的组合。包含一个或多个此类TEE的脂质的公式为(I):脂质基团-[疏水基团-pH敏感亲水基团](I)。该发明旨在提高脂质组装体的融合性。