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(-)-Epigallocatechin-3-gallate encapsulated realgar nanoparticles exhibit enhanced anticancer therapeutic efficacy against acute promyelocytic leukemia.
Drug Delivery ( IF 6 ) Pub Date : 2019-12-01 , DOI: 10.1080/10717544.2019.1672830
Wei Fang 1 , Zhao Liang Peng 2 , Ya Ji Dai 3 , Dian Lei Wang 1, 4 , Peng Huang 1 , He Ping Huang 1
Affiliation  

Realgar and (-)-Epigallocatechin-3-gallate (EGCG) are natural medicines that inhibit cancer cell growth, resulting in inhibition of formation and development of tumors. The anticancer effects of realgar and EGCG were greatly improved following formulation as nanoparticles. EGCG has received increased attention as a drug carrier. The aim of this study was to prepare a new nanomedicine, (EGCG-RNPs), in which encapsulated nano-realgar. EGCG-RNPs were prepared by coprecipitation and characterized by transmission electron microscopy (TEM), differential scanning calorimetry (DSC), particle size and zeta potential, X-ray diffraction, Fourier transform infrared spectroscopy (FTIR) and in vitro release. Furthermore, we evaluated the antiproliferative effects of EGCG-RNPs on HL-60 cells in vitro, antitumor effect by intratumoral injection of EGCG-RNPs into solid tumors derived from APL HL-60 cells in vivo. Possible mechanisms were evaluated using uptake and efflux experiments in HL-60 cells. The results showed that the average particle size and zeta potentials of EGCG-RNPs was 200.3 ± 1.23 nm and -46.8 ± 1.31 mV. Controlled release of EGCG-RNPs was sustained and continued up to 72 h in vitro. Compared with nano-realgar and EGCG + RNPs (EGCG and nano-realgar physical mixing), EGCG-RNPs significantly inhibited growth of HL-60 cells. In a solid tumor model, EGCG-RNPs decreased tumor volumes, with an inhibitory rate of 60.18% at a dose of 70 mg · kg-1. The mechanisms of antitumor improvement may correlate with the increased uptake of realgar and prolonged the retention time of realgar in HL-60 cells due to EGCG as a carrier. EGCG-RNPs could enhance anticancer therapeutic efficacy for acute promyelocytic leukemia.

中文翻译:

(-)-表没食子儿茶素-3-没食子酸酯包封的雄黄纳米颗粒表现出增强的针对急性早幼粒细胞白血病的抗癌治疗功效。

雄黄和(-)-Epigallocatechin-3-gallate(EGCG)是抑制癌细胞生长,抑制肿瘤形成和发展的天然药物。配制为纳米颗粒后,雄黄和EGCG的抗癌作用大大提高。EGCG作为药物载体已受到越来越多的关注。这项研究的目的是制备一种新的纳米药物(EGCG-RNPs),其中包封了纳米雄黄。EGCG-RNPs是通过共沉淀法制备的,并通过透射电子显微镜(TEM),差示扫描量热法(DSC),粒度和Zeta电位,X射线衍射,傅里叶变换红外光谱(FTIR)和体外释放来表征。此外,我们评估了EGCG-RNPs在体外对HL-60细胞的抗增殖作用,通过在体内将EGCG-RNPs肿瘤内注射到源自APL HL-60细胞的实体瘤中来产生抗肿瘤作用。使用在HL-60细胞中的摄取和外排实验评估了可能的机制。结果表明,EGCG-RNP的平均粒径和ζ电位为200.3±1.23nm和-46.8±1.31mV。EGCG-RNPs的控制释放在体外持续至72小时。与纳米雄激素和EGCG + RNPs(EGCG和纳米雄激素物理混合)相比,EGCG-RNPs显着抑制HL-60细胞的生长。在实体瘤模型中,EGCG-RNPs减少了肿瘤体积,在70 mg·kg-1的剂量下抑制率为60.18%。由于EGCG作为载体,抗肿瘤改善的机制可能与雄黄的摄取增加和雄黄在HL-60细胞中的保留时间延长有关。
更新日期:2019-11-18
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