Sarvagalla Sailu, Hsieh Hsing Pang, Coumar Mohane Selvaraj
a Centre for Bioinformatics, School of Life Sciences , Pondicherry University , Kalapet , Puducherry , India.
b Institute of Biotechnology and Pharmaceutical Research , National Health Research Institutes , Zhunan , Taiwan , ROC.
Expert Opin Ther Pat. 2016 Jul;26(7):751-5. doi: 10.1080/13543776.2016.1188919. Epub 2016 May 24.
Evaluation of the patent application WO2015036792 claiming therapeutic polymeric nanoparticles loaded with AZD1152-hqpa (aurora kinase inhibitor), and methods of making and using same for the treatment of cancer, is described. The claimed polymeric nano-formulations containing hydrophobic acid significantly improved the pharmacokinetic profiles (slow/sustained drug release profile) of the drug AZD1152-hqpa, as compared to the control agent (AZD1152). Drug efficacy and tolerability were also improved, and toxicity decreased in in vivo animal experiments, resulting in a better therapeutic index for the nano-formulation. Hence, the nano-formulated AZD1152-hqpa could be tested in the clinic at a dose level similar to, or higher than, that used for AZD1152, with lower incidence of toxicity.
本文描述了对专利申请WO2015036792的评估，该专利申请涉及负载AZD1152-hqpa（极光激酶抑制剂）的治疗性聚合物纳米颗粒及其制备方法和用于治疗癌症的用途。与对照剂（AZD1152）相比，所要求保护的含有疏水性酸的聚合物纳米制剂显著改善了药物AZD1152-hqpa的药代动力学特征（缓慢/持续药物释放曲线）。在体内动物实验中，药物疗效和耐受性也得到了改善，毒性降低，从而使纳米制剂具有更好的治疗指数。因此，纳米制剂的AZD1152-hqpa可以在临床上以与AZD1152相似或更高的剂量水平进行测试，且毒性发生率较低。
