Zhao Lai, Gu Xinquan, Jiang Fuquan, Li Bo, Lu Shuang, Wang Fan, Sun Yao, Liu Kai, Li Jingjing
Department of Urology, China-Japan Union Hospital of Jilin University, Changchun 130033, China.
State Key Laboratory of Rare Earth Resource Utilization, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China.
ACS Omega. 2022 Aug 24;7(35):31299-31308. doi: 10.1021/acsomega.2c03561. eCollection 2022 Sep 6.
Nanodrugs have attracted increasing interest in drug delivery and disease treatment. However, the cumbersome preparation process and the poor biocompatibility of nanodrugs obstruct their clinical translation. In this study, we utilized a self-assembly strategy to develop a low-toxicity, long-lasting nanodrug for the effective treatment and real-time monitoring of bladder tumors. The accurate self-assembly of compatible raw materials allowed for an encapsulation rate of 43.7% for insoluble erdafitinib. Interestingly, robust therapeutic effects and reduced side effects could be realized simultaneously using this nanodrug, enabling broader scenarios for the clinical application of erdafitinib. Furthermore, the nanodrug exhibited a significantly prolonged half-life (14.4 h) and increased bioavailability (8.0 μg/mL·h), which were 8.3 times and 5.0 times higher than those of its nonformulated counterpart. Also, it is worth mentioning that the introduction of a fluorescent protein module into the nanodrug brought up a novel possibility for real-time feedback on the therapeutic response. In conclusion, this research revealed a versatile technique for developing low-toxicity, long-acting, and multifunctional nanoformulations, paving the way for multidimensional therapy of malignant tumors.
纳米药物在药物递送和疾病治疗方面引起了越来越多的关注。然而，纳米药物繁琐的制备过程和较差的生物相容性阻碍了它们的临床转化。在本研究中，我们采用自组装策略开发了一种低毒性、长效的纳米药物，用于膀胱肿瘤的有效治疗和实时监测。兼容原料的精确自组装使得难溶性厄达替尼的包封率达到43.7%。有趣的是，使用这种纳米药物可以同时实现强大的治疗效果和减少的副作用，为厄达替尼的临床应用开辟了更广阔的前景。此外，该纳米药物的半衰期显著延长（14.4小时），生物利用度提高（8.0μg/mL·h），分别是非制剂对应物的8.3倍和5.0倍。同样值得一提的是，在纳米药物中引入荧光蛋白模块为治疗反应的实时反馈带来了新的可能性。总之，本研究揭示了一种开发低毒性、长效和多功能纳米制剂的通用技术，为恶性肿瘤的多维治疗铺平了道路。
