Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
本文介绍了通过将胺与环氧末端化合物反应制备
氨基醇脂质体的方法。还提供了从商业起始材料制备
氨基醇脂质体的方法。
氨基醇脂质体可以从外消旋或立体
化学纯的环氧化合物制备。
氨基醇脂质体或其盐形式最好是可
生物降解和
生物相容的,并可用于各种药物递送系统。由于这些
氨基醇脂质体化合物的
氨基基团,它们特别适用于多核苷酸的递送。已制备包含发明性脂质体和多核苷酸的复合物、胶束、脂质体或颗粒。发明性脂质体还可用于制备药物递送的微粒。鉴于它们缓冲其周围环境pH值的能力,它们特别适用于递送不稳定的药物。