[EN] LIPID ASSEMBLIES AND USES THEREOF AND SOME pH AND ELECTROSTATIC MODULATING LIPIDS TO BE USED IN SAID ASSEMBLIES<br/>[FR] ASSEMBLAGES LIPIDIQUES ET LEURS UTILISATIONS ET QUELQUES LIPIDES DE MODULATION DE PH ET ÉLECTROSTATIQUE DESTINÉS À ÊTRE UTILISÉS DANS LESDITS ASSEMBLAGES
申请人:YISSUM RES DEV CO
公开号:WO2016125163A1
公开(公告)日:2016-08-11
The present disclosure concerns modified lipid compounds and their use in the formation of lipid assemblies. Specifically are disclosed lipid assemblies comprising (a) an amphoteric lipid comprising in covalent association with (i) one or more acyl chains; (ii) one or more weak base moiety; (iii) one or more weak acid moiety; the lipid assembly also comprising (b) one or more additional lipids, at least one of which being a zwitterionic lipid. In some embodiments, the amphoteric lipid is a compound comprising (a) a tri-functional moiety; (b) two non-phosphate lipid chains associated with two of the functional moieties of said tri-functional moiety; (c) optionally a spacer moiety associated with the third of the functional moieties of said tri-functional moiety; and (d) a polyalkylamine optionally comprising a short peptide with one to several carboxylic acid residues. Also disclosed are the uses of the lipid assembly, inter alia, for transfection or cancer treatment.
本公开涉及改性脂质化合物及其在脂质组装中的应用。具体地,本公开揭示了包括(a)一种两性离子脂质,与之共价结合的包括(i)一个或多个酰基链;(ii)一个或多个弱碱基团;(iii)一个或多个弱酸基团;以及(b)一个或多个额外的脂质,其中至少一个是带电的两性离子脂质的脂质组装。在某些实施例中,两性离子脂质是一种化合物,包括(a)三官能团;(b)与三官能团中的两个官能团相关联的两个非磷脂质链;(c)可选地与三官能团中的第三个官能团相关联的间隔官能团;以及(d)一种聚烷基胺,可选地包括一个带有一到几个羧酸残基的短肽。本公开还揭示了脂质组装的用途,包括转染或癌症治疗等。