Poly(β-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings. A system for preparing and screening polymers in parallel using semi-automated robotic fluid delivery systems is also provided.
描述了通过双(仲胺)或
伯胺与双(
丙烯酸酯)共轭加成制备的聚(β-
氨基酯)。此外,还提供了用市售起始材料制备这些聚合物的方法。这些含叔胺的聚合物最好具有
生物降解性和
生物相容性,可用于各种给药系统。鉴于这些聚合物的聚(胺)性质,它们特别适合用于多核苷酸的递送。现已制备出含有聚合物/多核苷酸复合物的纳米颗粒。本发明的聚合物还可用于封装其他需要递送的制剂。由于它们能够缓冲周围环境的 pH 值,因此特别适用于递送易溶制剂。此外,还提供了一种利用半自动机器人流体输送系统平行制备和筛选聚合物的系统。