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Polymeric Lipid Hybrid Nanoparticles as a Delivery System Enhance the Antitumor Effect of Emodin in Vitro and in Vivo.

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机构: [1]College of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China [2]Guangdong Key Lab of Traditional Chinese Medicine Information Technology, College of Pharmacy, Jinan University, Guangzhou 510632, China [3]First Affiliated Hospital of Jinan University, Guangzhou 510630, China [4]College of Life Sciences, Liaoning University, Shenyang 110036, China [5]Cancer Research Institute of Jinan University, Guangzhou 510632, China
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关键词: Breast cancer Emodin Polymer lipid nanoparticles Anti-tumor activity

摘要:
This study aimed to evaluate the therapeutic efficacy of Emodin-loaded polymer lipid hybrid nanoparticles (E-PLNs) for breast cancer. The size, Zeta potential, surface morphology, encapsulation efficiency, stability, in vitro drug release of E-PLNs prepared by the nanoprecipitation method were characterized. The uptake, in-vitro cytotoxicities and apoptosis of free drug, E-PLNs were investigated against MCF-7 cells. The efficacy of E-PLNs in tumor bearing nude mice has also been studied.The average particle size of the experimentally prepared E-PLNs was (122.7±1.79) nm, and the encapsulation rate was 72.8%. Compared with free Emodin (EMO), E-PLNs showed greater toxicity to MCF-7 cells by promoting the uptake of EMO, and can promote the early apoptosis of MCF-7 cells. In addition to the morphological changes of apoptotic cells, the ratio of Bax/Bcl-2 was significantly increased, which indicated that E-PLNs can induce apoptosis in MCF-7 cells to achieve anticancer effect. Finally, E-PLNs significantly inhibited tumor growth by more than 60%, which may be related to its passive targeting effect on tumor site. Our results suggest that E-PLNs have shown good anti-breast cancer effect than free EMO. Moreover, the effect of E-PLNs on MCF-7 cells is mainly related to the induction of apoptosis. Copyright © 2021 American Pharmacists Association. Published by Elsevier Inc. All rights reserved.

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出版当年[2020]版:
大类 | 3 区 医学
小类 | 3 区 药物化学 3 区 药学 4 区 化学综合
最新[2025]版:
大类 | 3 区 医学
小类 | 3 区 药物化学 3 区 化学:综合 3 区 药学
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第一作者机构: [1]College of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China
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通讯机构: [1]College of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China [2]Guangdong Key Lab of Traditional Chinese Medicine Information Technology, College of Pharmacy, Jinan University, Guangzhou 510632, China [5]Cancer Research Institute of Jinan University, Guangzhou 510632, China [*1]College of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China.
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