Polyamidoamine conjugates containing curcumin and bisphosphonate were synthesized via a one-pot aqueous phase Michael addition reaction. In the design of the conjugate, bisphosphonate formed an integral part of the polymer carrier backbone. Curcumin was incorporated onto the polyamidoamine backbone via piperazine linker. The conjugates were characterized by Fourier transform spectroscopy, energy-dispersive X-ray analysis, atomic force spectroscopy and nuclear magnetic resonance spectroscopy and it confirmed the successful incorporation of the antiproliferative agents onto the carriers. The weight percentage incorporation of bisphosphonate to the carriers was found to be between 2.56% and 3.34%. The in vitro release studies of curcumin from the polyamidoamine conjugate were performed in dialysis bag at selected pH values. The release of curcumin was significantly slower at pH 7.4 when compared to pH 5.8. The release profiles indicate that the conjugates are more stable at pH 7.4 and are potential sustained drug-delivery systems for combination therapy.

中文翻译：

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聚酰胺酰胺共轭物的抗增殖剂的合成，表征和释放动力学。

通过一锅水相迈克尔加成反应合成了含有姜黄素和双膦酸酯的聚酰胺胺共轭物。在结合物的设计中，双膦酸酯形成了聚合物载体主链的组成部分。姜黄素通过哌嗪连接子掺入到聚酰胺酰胺主链上。通过傅立叶变换光谱，能量色散X射线分析，原子力光谱和核磁共振光谱对缀合物进行了表征，并证实了抗增殖剂已成功地掺入了载体中。发现双膦酸酯结合到载体中的重量百分比在2.56％和3.34％之间。在选定的pH值下，在透析袋中进行姜黄素从聚酰胺酰胺共轭物中的体外释放研究。与pH 5.8相比，姜黄素的释放在pH 7.4时明显较慢。释放曲线表明，缀合物在pH 7.4下更稳定，并且是用于联合治疗的潜在持续药物递送系统。