[EN] LIPIDS FOR DELIVERY OF CHARGED MATERIAL, FORMULATIONS THEREOF AND METHOD FOR MAKING SAME<br/>[FR] LIPIDES POUR L'ADMINISTRATION D'UN MATÉRIAU CHARGÉ, LEURS FORMULATIONS ET LEUR PROCÉDÉ DE FABRICATION
申请人:INTEGRATED NANOTHERAPEUTICS INC
公开号:WO2021026647A1
公开(公告)日:2021-02-18
Disclosed herein is a lipid having a net charge at physiological pH, and being covalently attached to a lipid moiety. The lipid moiety comprises a hydrocarbon structure having two or more linked hydrocarbon chains, optionally having cis or trans C=C, at least one of said chains being covalently attached to the head group optionally via the linker region. The hydrocarbon chains are bonded to one another at a branch point at an internal carbon of the chain attached to the linker region, which branch point comprises a functional group having an electronegative atom. The hydrocarbon chains each have between 1 and 40 carbon atoms, wherein the hydrocarbon structure in total comprises between 10 and 150 carbon atoms. Advantageously, the hydrocarbon structure may assume a generally flared shape for enhanced delivery of cargo molecules. Further provided are delivery vehicles comprising the lipids.
本文揭示了一种在生理pH下具有净电荷的脂质,且与脂质部分共价连接。脂质部分包括具有两个或更多个连接的碳氢链的碳氢结构,可选择具有顺式或反式C=C,其中至少一个链通过连接区域共价连接到头基。碳氢链在连接到连接区域的链的内部碳上相互连接在一个分支点上,该分支点包括具有电负原子的功能基团。每个碳氢链具有1至40个碳原子,其中总的碳氢结构包括10至150个碳原子。优点是,碳氢结构可以呈现一种通常呈扩张形状以增强货物分子的输送。此外,提供了包含这些脂质的输送载体。