Metal-organic framework IRMOFs coated with a temperaturesensitive gel delivering norcantharidin to treat liver cancer  

作　　者：Xiu-Yan Li Qing-Xia Guan Yu-Zhou Shang Yan-Hong Wang Shao-Wa Lv Zhi-Xin Yang Rui Wang Yu-Fei Feng Wei-Nan Li Yong-Ji Li 

机构地区：[1]College of Pharmacy,Heilongjiang University of Chinese Medicine,Harbin 150040,Heilongjiang Province,China

出　　处：《World Journal of Gastroenterology》2021年第26期4208-4220,共13页世界胃肠病学杂志（英文版）

基　　金：Supported by National Natural Science Foundation of China,No.82074025 and No.82074271;the Heilongjiang Traditional Chinese Medicine Research Project,No.ZHY18-047;and Scientific Research Project of Heilongjiang Health Committee,No.2020-293.

摘　　要：BACKGROUND Norcantharidin(NCTD)is suitable for the treatment of primary liver cancer,especially early and middle primary liver cancer.This compound can reduce tumors and improve immune function.However,the side effects of NCTD have limited its application.There is a marked need to reduce the side effects and increase the efficacy of NCTD.AIM To develop a nanomaterial carrier,NCTD-loaded metal-organic framework IRMOF-3 coated with a temperature-sensitive gel(NCTD-IRMOF-3-Gel),aiming to improve the anticancer activity of NCTD and reduce the drug dose.METHODS NCTD-IRMOF-3-Gel was obtained by a coordination reaction.The apparent characteristics and in vitro release of NCTD-IRMOF-3-Gel were investigated.Cell cytotoxicity assays,flow cytometry,and apoptosis experiments in mouse hepatoma(Hepa1-6)cells were used to determine the anti-liver cancer activity of NCTD-IRMOF-3-Gel in in vitro models.RESULTS The particle size of NCTD-IRMOF-3-Gel was 50-100 nm,and the particle size distribution was uniform.The release curve showed that NCTD-IRMOF-3-Gel had an obvious sustained-release effect.The cytotoxicity assays showed that the free drug NCTD and NCTD-IRMOF-3-Gel treatments markedly inhibited Hepa1-6 cell proliferation,and the inhibition rate increased with increasing drug concentration.By flow cytometry,NCTD-IRMOF-3-Gel was observed to block the Hepa1-6 cell cycle in the S and G2/M phases,and the thermosensitive gel nanoparticles may inhibit cell proliferation by inducing cell cycle arrest.Apoptosis experiments showed that NCTD-IRMOF-3-Gel induced the apoptosis of Hepa1-6 cells.CONCLUSION Our results indicated that the NCTD-IRMOF-3-Gel may be beneficial for liver cancer disease treatment.

关 键 词：NORCANTHARIDIN Metal-organic frameworks IRMOF-3 Temperature-sensitive gel Drug delivery Liver cancer 

分 类 号：R735.7[医药卫生—肿瘤]