Andrianov Alexander K, Marin Alexander, Chen Jianping
Parallel Solutions Incorporated, 763D Concord Avenue, Cambridge, MA 02138, USA.
Biomacromolecules. 2006 Jan;7(1):394-9. doi: 10.1021/bm050790a.
A new water-soluble polyphosphazene polyelectrolyte containing carboxylate functionalities, poly[di(sodium carboxylatoethylphenoxy)phosphazene] (PCEP) was synthesized via reaction of macromolecular substitution. The polymer was characterized using (1)H, (31)P NMR, and gel permeation chromatography with multiangle laser light scattering detection. PCEP was shown to undergo hydrolytic degradation in aqueous solutions, as indicated by the decrease in the molecular weight and the release of side groups. A series of incompletely substituted copolymers of PCEP containing varying amounts of residual chlorine atoms was also prepared. The rate of degradation for such copolymers increased with the rise in the content of chlorine atoms. In vivo studies demonstrated high potency of PCEP as a vaccine immunoadjuvant. The new polyphosphazene was also shown to be capable of forming microspheres in aqueous solutions via reactions of ionic complexation with physiologically occurring amines, such as spermine.
通过大分子取代反应合成了一种新型的含羧酸盐官能团的水溶性聚磷腈聚电解质，聚[二（羧基乙氧基苯氧基）磷腈钠]（PCEP）。使用（1）H、（31）P NMR以及带有多角度激光光散射检测的凝胶渗透色谱法对该聚合物进行了表征。如分子量的降低和侧基的释放所示，PCEP在水溶液中会发生水解降解。还制备了一系列含有不同量残留氯原子的PCEP不完全取代共聚物。此类共聚物的降解速率随氯原子含量的增加而加快。体内研究表明PCEP作为疫苗免疫佐剂具有高效性。这种新型聚磷腈还显示出能够通过与生理上存在的胺（如精胺）进行离子络合反应在水溶液中形成微球。
