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柚皮素载药纳米粒延缓大鼠肝癌的发展。

Apigenin loaded nanoparticle delayed development of hepatocellular carcinoma in rats.

机构信息

Department of Pharmaceutical Technology, Jadavpur University, Kolkata, West Bengal, India.

Department of Pharmaceutical Technology, Jadavpur University, Kolkata, West Bengal, India.

出版信息

Nanomedicine. 2018 Aug;14(6):1905-1917. doi: 10.1016/j.nano.2018.05.011. Epub 2018 May 23.

DOI:10.1016/j.nano.2018.05.011
PMID:29802937
Abstract

Hepatocellular carcinoma (HCC) is one of the major causes of cancer related death globally. Apigenin, a dietary flavonoid, possesses anti-tumor activity against HCC cells in-vitro. Development, physicochemical characterization of apigenin loaded nanoparticles (ApNp), biodistribution pattern and pharmacokinetic parameters of apigenin upon intravenous administration of ApNp, and effect of ApNp treatment in rats with HCC were investigated. Apigenin loaded nanoparticles had a sustained drug release pattern and successfully reached the hepatic cancer cells in-vitro as well as in liver of carcinogenic animals. ApNp predominantly delayed the progress of HCC in chemical induced hepatocarcinogenesis in rats. Quantification of apigenin by liquid chromatography-mass spectroscopy (LC-MS/MS) showed that apigenin availability significantly increased in blood and liver upon ApNp treatment. Apigenin loaded nanoparticle delivery substantially controlled the severity of hepatocellular carcinoma and could be a future hope for lingering the survival in hepatic cancer patients.

摘要

肝细胞癌 (HCC) 是全球癌症相关死亡的主要原因之一。芹菜素是一种膳食类黄酮,具有体外抗肝癌细胞的抗肿瘤活性。本研究旨在探索芹菜素负载纳米粒 (ApNp) 的开发、理化特性、体内分布模式和药代动力学参数,以及 ApNp 治疗荷 HCC 大鼠的效果。研究发现,ApNp 具有持续的药物释放模式,可成功递送到体外肝癌细胞以及致癌动物的肝脏中。ApNp 主要延缓了化学诱导的大鼠肝癌发生过程中的 HCC 进展。通过液相色谱-质谱联用 (LC-MS/MS) 定量分析表明,ApNp 治疗后血液和肝脏中芹菜素的含量显著增加。ApNp 纳米粒给药可显著控制肝癌的严重程度,为延长肝癌患者的生存带来新的希望。

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