Nottelet B, El Ghzaoui A, Coudane J, Vert M
Max Mousseron Institute on Biomolecules, UMR CNRS 5247, Faculty of Pharmacy, 15, Avenue Charles Flahault, BP 14491, 34093 Montpellier cedex 5, France.
Biomacromolecules. 2007 Aug;8(8):2594-601. doi: 10.1021/bm700449c. Epub 2007 Jul 11.
As part of the search of novel degradable polymers, amphiphilic and cationic poly(epsilon-caprolactone)-g-poly(l-lysine) (PCL-g-PlL) copolymers have been synthesized following a grafting "onto" or a grafting "from" method both applied to a macropolycarbanionic PCL derivative. The first approach led to PCL-g-PZlL containing 36% of epsilon-caprolactone and 64% of N-epsilon-Z-l-lysine units, by reaction of activated poly(N-epsilon-Z-l-lysine) on the macropolycarbanion derived from PCL. The second route was based on the anionic ring opening polymerization of N-carboxyanhydride of N-epsilon-benzyloxycarbonyl-l-lysine initiated by the macropolycarbanion derived from PCL and led to a similar copolymer containing 45% of of epsilon-caprolactone and 55% of N-epsilon-Z-l-lysine units. After deprotection of the lysine units, PCL-g-PlL copolymers were obtained. These copolymers are water-soluble and form nanometric micelle-like objects with mean diameters between 60 and 500 nm in distilled water depending on the synthesis route.
作为新型可降解聚合物研究的一部分,通过“接枝到”或“从……接枝”方法合成了两亲性和阳离子型聚(ε-己内酯)-g-聚(L-赖氨酸)(PCL-g-PlL)共聚物,这两种方法均应用于一种大分子聚碳阴离子型PCL衍生物。第一种方法是通过活化的聚(N-ε-Z-L-赖氨酸)与由PCL衍生的大分子聚碳阴离子反应,得到含有36%的ε-己内酯和64%的N-ε-Z-L-赖氨酸单元的PCL-g-PZlL。第二条路线基于由PCL衍生的大分子聚碳阴离子引发的N-ε-苄氧羰基-L-赖氨酸的N-羧基酐的阴离子开环聚合,得到了一种类似的共聚物,其中含有45%的ε-己内酯和55%的N-ε-Z-L-赖氨酸单元。赖氨酸单元脱保护后,得到了PCL-g-PlL共聚物。这些共聚物是水溶性的,在蒸馏水中形成平均直径在60至500纳米之间的纳米级胶束状物体,这取决于合成路线。