Andrianov Alexander K, Svirkin Yuri Y, LeGolvan Mark P
Parallel Solutions Inc., 763D Concord Avenue, Cambridge, Massachusetts 02138, USA.
Biomacromolecules. 2004 Sep-Oct;5(5):1999-2006. doi: 10.1021/bm049745d.
Polyphosphazene polyacids show potential as immunostimulating compounds and materials for microencapsulation. Their synthesis requires multistep chemical transition from a hydrolytically unstable macromolecular precursor, poly(dichlorophosphazene), to a water-soluble polyelectrolyte. Insufficient synthetic control in these reactions can lead to molecular weight variations and formation of macromolecules with "structural defects" resulting in significant variations in polymer performance. Simple and reproducible "one pot-one solvent" method is reported for the preparation of polyphosphazene polyacids-poly[di(carboxylatophenoxy)phosphazene] and its copolymers. Molecular weight characteristics and polymer compositions were studied as a function of reaction parameters. Macromolecular byproducts, incompletely substituted polymers containing hydroxyl groups and partially deprotected polymers containing propyl ester functionalities, were synthesized and characterized. It was demonstrated, that the presence of such groups can affect polymer characteristics, such as hydrolytic degradation profiles, immunostimulating activity, and microsphere forming properties. In vivo studies showed that the immunostimulating activity of polyphosphazene polyacids correlates with the content of acid functionalities in the polymer.
聚磷腈聚酸作为免疫刺激化合物和微囊化材料具有潜力。它们的合成需要从水解不稳定的大分子前体聚（二氯磷腈）进行多步化学转变，生成水溶性聚电解质。这些反应中合成控制不足会导致分子量变化以及形成具有“结构缺陷”的大分子，从而导致聚合物性能出现显著差异。本文报道了一种简单且可重现的“一锅一溶剂”方法来制备聚磷腈聚酸——聚[二（羧基苯氧基）磷腈]及其共聚物。研究了分子量特征和聚合物组成与反应参数的关系。合成并表征了大分子副产物、含有羟基的未完全取代聚合物以及含有丙酯官能团的部分脱保护聚合物。结果表明，这些基团的存在会影响聚合物特性，如水解降解曲线、免疫刺激活性和微球形成性能等。体内研究表明，聚磷腈聚酸的免疫刺激活性与聚合物中酸性官能团的含量相关。
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