申请人:Massachusetts Institute of Technology
公开号:EP2476756A1
公开(公告)日:2012-07-18
Nitrogen-containing lipids prepared from the conjugate addition of amines to acrylates, acrylamides, or other carbon-carbon double bonds conjugated to electron-withdrawing groups are described. Methods of preparing these lipids from commercially available starting materials are also provided. These amine-containing lipids or salts forms of these lipids are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these lipids, they are particularly suited for the delivery of polynucleotides. Complexes or nanoparticles containing the inventive lipid and polynucleotide have been prepared. The inventive lipids may also be used to in preparing microparticle for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
本文介绍了通过胺与丙烯酸酯、丙烯酰胺或其他与电子萃取基团共轭的碳碳双键的共轭加成制备含氮脂质的方法。此外,还提供了利用市售起始材料制备这些脂质的方法。这些含胺脂质或其盐类最好具有生物降解性和生物相容性,可用于各种给药系统。考虑到这些脂质的氨基,它们特别适用于多核苷酸的递送。已制备出含有本发明脂质和多核苷酸的复合物或纳米颗粒。本发明脂质还可用于制备给药微粒。由于本发明脂质具有缓冲周围环境 pH 值的能力,因此特别适用于递送易溶剂。