甲氨蝶呤和β-胡萝卜素负载脂质聚合物杂化纳米粒：用于乳腺癌的临床前研究。
Methotrexate and beta-carotene loaded-lipid polymer hybrid nanoparticles: a preclinical study for breast cancer.
机构信息
University Institute of Pharmaceutical Sciences, UGC-Centre of Advanced Studies, Panjab University, Chandigarh 160 014, India.
UGC-Centre of Excellence in Applications of Nanomaterials, Nanoparticles & Nanocomposites, Panjab University, Chandigarh 160 014, India.
出版信息
Nanomedicine (Lond). 2017 Aug;12(15):1851-1872. doi: 10.2217/nnm-2017-0011. Epub 2017 Jul 13.
AIM
This work was intended to investigate the targeting potential of fructose-tethered lipid-polymeric hybrid nanoparticles (F-BC-MTX-LPHNPs) co-loaded with beta carotene (BC) and methotrexate (MTX) in breast cancer therapeutics and find out the possible protective role of BC on MTX-induced toxicity.
MATERIALS & METHODS: F-BC-MTX-LPHNPs were fabricated using self-assembled nano-precipitation technique. Fructose was conjugated on the surface of the particles. The in vitro cytotoxicity, sub-cellular localization and apoptotic activity of F-BC-MTX-LPHNPs were evaluated against MCF-7 breast cancer cells. The antitumor potential of F-BC-MTX-LPHNPs was further studied.
RESULTS & CONCLUSION: Outcomes suggested that F-BC-MTX-LPHNPs induced the highest apoptosis index (0.89) against MCF-7 cells. Following 30 days of treatment, the residual tumor progression was assessed to be approximately 32%, in animals treated with F-BC-MTX-LPHNPs. F-BC-MTX-LPHNPs are competent to selectively convey the chemotherapeutic agent to the breast cancers. Beta carotene ameliorated MTX-induced hepatic and renal toxicity.
目的
本研究旨在探讨同时载有β-胡萝卜素（BC）和甲氨蝶呤（MTX）的果糖连接的脂质-聚合物杂化纳米粒（F-BC-MTX-LPHNPs）在乳腺癌治疗中的靶向潜力，并发现 BC 对 MTX 诱导的毒性可能具有的保护作用。
材料与方法
采用自组装纳米沉淀技术制备 F-BC-MTX-LPHNPs。将果糖偶联到颗粒表面。用 MCF-7 乳腺癌细胞评价 F-BC-MTX-LPHNPs 的体外细胞毒性、亚细胞定位和凋亡活性。进一步研究了 F-BC-MTX-LPHNPs 的抗肿瘤潜力。
结果与结论
结果表明，F-BC-MTX-LPHNPs 对 MCF-7 细胞诱导的凋亡指数最高（0.89）。治疗 30 天后，用 F-BC-MTX-LPHNPs 治疗的动物的残余肿瘤进展评估约为 32%。F-BC-MTX-LPHNPs 能够选择性地将化疗药物递送到乳腺癌中。β-胡萝卜素改善了 MTX 诱导的肝肾功能毒性。
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