Forte Gianpiero, Chiarotto Isabella, Giannicchi Ilaria, Loreto Maria Antonietta, Martinelli Andrea, Micci Roberta, Pepi Federico, Rossi Serena, Salvitti Chiara, Stringaro Annarita, Tortora Luca, Vecchio Ciprioti Stefano, Feroci Marta
a Dipartimento di Scienze di Base e Applicate per l'Ingegneria , Sapienza Università di Roma , Roma , Italy.
b Dipartimento di Chimica , Sapienza Università di Roma , Roma , Italy.
J Biomater Sci Polym Ed. 2016;27(1):69-85. doi: 10.1080/09205063.2015.1108637. Epub 2015 Nov 7.
The synthesis and the characterization of three new naproxen decorated polymers are described. A versatile and general approach is employed to link the drug to polymers, affording the derivatives with a very high degree of purity. The release of the drug from the conjugates proved to be exceptionally slow, even in acidic aqueous media, and the kinetic of the process seems to be triggered by their solubility in water. On the other hand, the interesting outcome of the first ex vivo drug release experiments on human blood samples makes this preliminary study valuable for future investigations on the use of these polymeric prodrugs in in vivo treatment of inflammatory states.
描述了三种新型萘普生修饰聚合物的合成与表征。采用了一种通用且灵活的方法将药物连接到聚合物上，得到了具有极高纯度的衍生物。即使在酸性水性介质中，药物从缀合物中的释放也被证明异常缓慢，并且该过程的动力学似乎由它们在水中的溶解度触发。另一方面，首次对人体血液样本进行的体外药物释放实验取得的有趣结果，使得这项初步研究对于未来关于这些聚合物前药在体内炎症状态治疗中的应用研究具有重要价值。
