将多柔比星和 4-硝基查尔酮载入蜂蜡基纳米结构脂质载体:体外抗肿瘤筛选以及对 HepG-2 细胞协同作用的评估。

IF 6 2区 医学 Q1 PHARMACOLOGY & PHARMACY International Journal of Pharmaceutics Pub Date : 2024-12-05 Epub Date: 2024-10-03 DOI:10.1016/j.ijpharm.2024.124788
Arthur Poester Cordeiro , Paulo Emílio Feuser , Pedro H.H. Araújo , Daniela Coelho dos Santos , Fabiana Ourique , Luiza Johanna Hübner , Rozangela Curi Pedrosa , Claudia Sayer
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引用次数: 0

摘要

癌症是全球第二大致命疾病,而化疗等最传统的方法仍然面临着药物剂量和脱靶副作用的限制。为了解决这些问题,我们提出了使用蜂蜡基纳米结构脂质载体(NLCs)同时给药 4-硝基查尔酮(4NC)和多柔比星(DOX)的方案。采用水/油/水双乳液技术和熔融分散方法,在蜂蜡基纳米脂质载体中实现了 4NC 和 DOX 的共包囊。该体系由平均直径约为 200 nm 的半球形 NLC 组成,粒度分布较窄,在再分散前后均表现出胶体稳定性,zeta 电位保持在 -30 mV 以下。在不同的肿瘤细胞系上对纳米颗粒的抗肿瘤活性进行了筛选,并对肝癌细胞的诱导细胞死亡和内部 ROS 水平进行了分析,发现 4NC 和 DOX 的组合对肝癌细胞的影响更大。结果表明,4NC + DOX-NCLs 可促进 HepG-2 细胞系的细胞毒性和氧化损伤介导的细胞凋亡。
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Doxorubicin and 4-nitrochalcone loaded in beeswax-based nanostructured lipid carriers: In vitro antitumoral screening and evaluation of synergistic effect on HepG-2 cells
Cancer is the second most deadly disease worldwide, and the most traditional approaches such as chemotherapy still face limitations associated to drug dosage and off-target side effects. To address these issues, we propose the simultaneous administration of 4-Nitrochalcone (4NC) and Doxorubicin (DOX) using beeswax based nanostructured lipid carriers (NLCs). The co-encapsulation of 4NC and DOX in the beeswax based NLCs was performed using the water/oil/water double emulsion technique in association with the melt dispersion approach. The system composed by semi-spherical NLCs with an average diameter around 200 nm and narrow size distribution, displayed colloidal stability before and after redispersion, keeping the zeta potential below −30 mV. The antitumor activity of the nanoparticles was screened on different tumor cell lines, and the induced cellular death and internal ROS levels were analyzed on hepatocarcinoma cells, which were found to be more affected by the combination of 4NC and DOX. The results indicated that 4NC + DOX-NCLs could promote cytotoxicity and oxidative damage-mediated apoptosis in a HepG-2 cell line.
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来源期刊
CiteScore
10.70
自引率
8.60%
发文量
951
审稿时长
72 days
期刊介绍: The International Journal of Pharmaceutics is the third most cited journal in the "Pharmacy & Pharmacology" category out of 366 journals, being the true home for pharmaceutical scientists concerned with the physical, chemical and biological properties of devices and delivery systems for drugs, vaccines and biologicals, including their design, manufacture and evaluation. This includes evaluation of the properties of drugs, excipients such as surfactants and polymers and novel materials. The journal has special sections on pharmaceutical nanotechnology and personalized medicines, and publishes research papers, reviews, commentaries and letters to the editor as well as special issues.
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