Institute of Polymers, Bulgarian Academy of Sciences, Sofia 1113, Bulgaria.
A.N. Nesmeyanov Institute of Organoelement Compounds of Russian Academy of Sciences, Moscow 119991, Russia.
Biomacromolecules. 2021 Feb 8;22(2):971-983. doi: 10.1021/acs.biomac.0c01666. Epub 2020 Dec 28.
Novel N-substituted polyacrylamides bearing a cycle with two tertiary amines, poly(4-methyl-piperazin-1-yl)-propenone (PMPP) and its block copolymers with polylactide (PMPP--PLA), are synthesized and characterized. The homopolymers are water-soluble, whereas the block copolymers self-assemble in aqueous solution into a small size ( around 30 nm), are narrowly distributed, and exhibit core-shell micelles with good colloidal stability. Both the homopolymers and copolymer micelles are positively charged (ζ-potentials in the 13.8-17.6 mV range), which are employed for formation of electrostatic complexes with oppositely charged DNA. Complexes (polyplexes, micelleplexes, and spherical nucleic acidlike structures) in a wide range of N/P (amino to phosphate groups) ratios are prepared with short (115 bp) and long (2000 bp) DNA. The behavior and physicochemical properties of the resulting nanocarriers of DNA are strongly dependent on the polymer/polymer micelles' characteristics and the DNA chain length. All systems exhibit low cytotoxicity and good cellular uptake ability and show promise for gene delivery and regulation.
合成并表征了含有两个叔胺的新型 N-取代的聚丙烯酰胺，即聚（4-甲基哌嗪-1-基）丙烯酮（PMPP）及其与聚乳酸（PMPP-PLA）的嵌段共聚物。均聚物可溶于水，而嵌段共聚物在水溶液中自组装成小尺寸（约 30nm）、分布窄的核壳型胶束，具有良好的胶体稳定性。均聚物和共聚物胶束均带正电荷（ζ-电位在 13.8-17.6mV 范围内），可与带相反电荷的 DNA 形成静电复合物。用短链（115bp）和长链（2000bp）DNA 制备了 N/P（氨基与磷酸基团）比在很宽范围内的复合物（多聚物复合物、胶束复合物和球形核酸样结构）。所得 DNA 的纳米载体的行为和物理化学性质强烈依赖于聚合物/聚合物胶束的特性和 DNA 链长。所有系统均表现出低细胞毒性和良好的细胞摄取能力，有望用于基因传递和调控。
