生物利用度
药效学
体内
氯硝柳胺
环糊精
化学
细胞凋亡
体外
药理学
溶解度
核化学
医学
色谱法
药代动力学
生物
生物化学
有机化学
生物技术
生态学
作者
Lukuan Liu,Yu Chen,Liwen Chen,Yuyang Shi,Jiqin Fang,Min Zhao,Miao Wang
标识
DOI:10.1016/j.jddst.2022.104031
摘要
Niclosamide (NIC) has been found to have good antitumor activity in recent years, but its poor water solubility has limited its use in the treatment of tumors. In this study, NIC-Hydroxypropyl-β-cyclodextrin inclusion complex (NHC) was prepared to improve the solubility and bioavailability of NIC. X-ray diffraction (XRD) analysis of the NHC showed that the NHC was successfully prepared. The NIC standard curve was then established by UV spectrophotometry and the encapsulation rate of the NHC was examined and the encapsulation rate of NHC was 81.05%. The therapeutic effects of NIC and NHC on breast cancer were compared by in vivo and in vitro experiments. In the in vitro experiments, we performed MTT, apoptosis, and cell cycle assays, and the results showed that NHC was able to promote apoptosis and block the G2/M phase better than NIC. The tumour inhibition rate of NIC was 39.99% and that of NHC was 49.76%, which showed a significant reduction in tumors. There was also a reduction in lung metastasis after NHC inclusion treatment compared to NIC. Histopathological sections also showed significant improvement in symptoms after administration. In conclusion, the NHC is a potentially effective treatment for breast cancer compared to NIC.
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