FLQY2 is a camptothecin derivative modified by FL118 and proved to be good antitumor activity in vitro. However, its poor solubility leads to the low therapeutic efficacy in vivo. Here, the injectable FLQY2 lyophilized powder was prepared with Kolliphor® HS 15 (HS 15), which was called HS 15-FLQY2. The preparation process of HS 15-FLQY2 was optimized by orthogonal design and the lyophilization process was investigated by single factor experiment. Moreover, the formulation was characterized, the pharmacokinetics study and the antitumor activity were carried out in vivo. As the results, HS 15-FLQY2 (1:1500, w/w) containing 5% mannitol as cryoprotectant showed good appearance and 70% entrapment efficiency. HS 15-FLQY2 revealed low particle size (<16 nm), better homogeneity (PDI <0.2) and remained stable for 24 h in water. In addition, the data of the DSC, XRD and FTIR demonstrated that FLQY2 was distributed within micelles. In vivo, the bioavailability of HS 15-FLQY2 (i.p.) was improved significantly compared with oral CD-FLQY2 (a cyclodextrin inclusion complex of FLQY2). In addition, HS 15-FLQY2 demonstrated higher tumor inhibition effect than capecitabine, confirming the possibility of treatment cancer by the delivery of FLQY2.

FLQY2是由FL118修饰的喜树碱衍生物，经体外证明具有良好的抗肿瘤活性。然而，其溶解性差导致体内治疗效果低下。在这里，注射用 FLQY2 冻干粉是用 Kolliphor® HS 15 (HS 15) 制备的，称为 HS 15-FLQY2。通过正交设计优化了HS 15-FLQY2的制备工艺，并通过单因素实验研究了冻干工艺。此外，在体内进行了制剂表征、药代动力学研究和抗肿瘤活性研究。. 结果，含有 5% 甘露醇作为冷冻保护剂的 HS 15-FLQY2 (1:1500, w/w) 表现出良好的外观和 70% 的包封率。HS 15-FLQY2 显示出低粒径 (<16 nm)、更好的均匀性 (PDI <0.2) 并在水中保持稳定 24 小时。此外，DSC、XRD和FTIR的数据表明FLQY2分布在胶束内。在体内，与口服 CD-FLQY2（FLQY2 的环糊精包合物）相比，HS 15-FLQY2 (ip) 的生物利用度显着提高。此外，HS 15-FLQY2 表现出比卡培他滨更高的肿瘤抑制作用，证实了通过递送 FLQY2 治疗癌症的可能性。