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青蒿琥酯负载及甘草次酸包被纳米粒的肝靶向性及抗肝癌活性评价

Evaluation of the liver targeting and anti‑liver cancer activity of artesunate‑loaded and glycyrrhetinic acid‑coated nanoparticles.

作者信息

Pan Xu-Wang, Huang Jin-Song, Liu Shou-Rong, Shao Yi-Dan, Xi Jian-Jun, He Ruo-Yu, Shi Ting-Ting, Zhuang Rang-Xiao, Bao Jian-Feng

机构信息

Department of Pharmaceutical Preparation, Hangzhou Xixi Hospital, Hangzhou, Zhejiang 310023, P.R. China.

Department of Liver Disease, Hangzhou Xixi Hospital, Hangzhou, Zhejiang 310023, P.R. China.

出版信息

Exp Ther Med. 2023 Sep 21;26(5):516. doi: 10.3892/etm.2023.12215. eCollection 2023 Nov.

DOI:10.3892/etm.2023.12215
PMID:37854499
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10580252/
Abstract

Globally, liver cancer ranks among the most lethal cancers, with chemotherapy being one of its primary treatments. However, poor selectivity, systemic toxicity, a narrow treatment window, low response rate and multidrug resistance limit its clinical application. Liver-targeted nanoparticles (NPs) exhibit excellent targeted delivery ability and promising effectivity in treating liver cancer. The present study aimed to investigate the liver-targeting and anti-liver cancer effect of artesunate (ART)-loaded and glycyrrhetinic acid (GA)-decorated polyethylene glycol (PEG)-poly (lactic-co-glycolic acid) (PLGA) (ART/GA-PEG-PLGA) NPs. GA-coated NPs significantly increased hepatoma-targeted cellular uptake, with micropinocytosis and caveolae-mediated endocytosis as its chief internalization pathways. Moreover, ART/GA-PEG-PLGA NPs exhibited pro-apoptotic effects on HepG2 cells, mainly via the induction of a high level of reactive oxygen species, decline in mitochondrial membrane potential and induction of cell cycle arrest. Additionally, ART/GA-PEG-PLGA NPs induced internal apoptosis pathways by upregulating the activity of cleaved caspase-3/7 and expression of cleaved poly (ADP-Ribose)-polymerase and Phos-p38 mitogen-activated protein kinase in HepG2 cells. Furthermore, ART/GA-PEG-PLGA NPs exhibited higher liver accumulation and longer mean retention time, resulting in increased bioavailability. Finally, ART/GA-PEG-PLGA NPs promoted the liver-targeting distribution of ART, increased the retention time and promoted its antitumour effects . Therefore, ART/GA-PEG-PLGA NPs afforded excellent hepatoma-targeted delivery and anti-liver cancer efficacy, and thus, they may be a promising strategy for treating liver cancer.

摘要

在全球范围内，肝癌是最致命的癌症之一，化疗是其主要治疗方法之一。然而，化疗的选择性差、全身毒性、治疗窗口窄、反应率低和多药耐药性限制了其临床应用。肝靶向纳米颗粒（NPs）在治疗肝癌方面表现出优异的靶向递送能力和良好的有效性。本研究旨在探讨负载青蒿琥酯（ART）和甘草次酸（GA）修饰的聚乙二醇（PEG）-聚（乳酸-乙醇酸）（PLGA）（ART/GA-PEG-PLGA）纳米颗粒的肝靶向性和抗肝癌作用。GA包被的纳米颗粒显著增加了肝癌靶向细胞摄取，以微胞饮作用和小窝介导的内吞作用为主要内化途径。此外，ART/GA-PEG-PLGA纳米颗粒对HepG2细胞具有促凋亡作用，主要通过诱导高水平的活性氧、线粒体膜电位下降和诱导细胞周期停滞。此外，ART/GA-PEG-PLGA纳米颗粒通过上调HepG2细胞中裂解的caspase-3/7活性、裂解的聚（ADP-核糖）-聚合酶和磷酸化p38丝裂原活化蛋白激酶的表达来诱导内源性凋亡途径。此外，ART/GA-PEG-PLGA纳米颗粒表现出更高的肝脏蓄积和更长的平均滞留时间，从而提高了生物利用度。最后，ART/GA-PEG-PLGA纳米颗粒促进了ART的肝靶向分布，延长了滞留时间并促进了其抗肿瘤作用。因此，ART/GA-PEG-PLGA纳米颗粒提供了优异的肝癌靶向递送和抗肝癌疗效，因此，它们可能是治疗肝癌的一种有前途的策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/fecccab369bb/etm-26-05-12215-g08.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/32319ff41a43/etm-26-05-12215-g00.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/d82836429741/etm-26-05-12215-g01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/505fd2ab46fe/etm-26-05-12215-g02.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/40e796c87aaf/etm-26-05-12215-g03.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/2ae920f5e799/etm-26-05-12215-g04.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/a0e8bf752ae4/etm-26-05-12215-g05.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/19c43c5f5b50/etm-26-05-12215-g06.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/f1aafd66bbd3/etm-26-05-12215-g07.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/fecccab369bb/etm-26-05-12215-g08.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/32319ff41a43/etm-26-05-12215-g00.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/d82836429741/etm-26-05-12215-g01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/505fd2ab46fe/etm-26-05-12215-g02.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/40e796c87aaf/etm-26-05-12215-g03.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/2ae920f5e799/etm-26-05-12215-g04.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/a0e8bf752ae4/etm-26-05-12215-g05.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/19c43c5f5b50/etm-26-05-12215-g06.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/f1aafd66bbd3/etm-26-05-12215-g07.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c2e5/10580252/fecccab369bb/etm-26-05-12215-g08.jpg

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