Department of Molecular Biology and Genetics, Faculty of Arts and Science, Yildiz Technical University, Istanbul, Turkey.
J Microencapsul. 2021 Sep;38(6):381-393. doi: 10.1080/02652048.2021.1948623. Epub 2021 Jul 5.
This study aimed to synthesise quercetin- caffeic-acid phenethyl ester (CAPE)-co-loaded poly(lactic-co-glycolic-acid) (PLGA) nanoparticles (QuCaNP) and investigate their anti-cancer activity on human colorectal carcinoma HT-29 cells.
QuCaNPs were synthesised using single-emulsion (o/w) solvent evaporation method. Particle size, zeta potential, polydispersity index, release profile, and surface morphology of QuCaNPs were determined. Cytotoxicity, anti-migration, anti-proliferation and apoptotic activities of QuCaNPs were studied.
Mean diameter of QuCaNP was 237.8 ± 9.670 nm, with a polydispersity index (PDI) of 0.340 ± 0.027. Encapsulation efficiency was 74.28% (quercetin) and 65.24% (CAPE). Particle size and drug content of QuCaNP remained stable for 30 days at -20 °C. The half-maximal inhibitory concentration (IC) values of QuCaNP-treated HT-29 cells were calculated as 11.2 µg/mL (24 h) and 8.2 µg/mL (48 h). QuCaNP treatment increased mRNA levels of caspase-3 (2.38 fold) and caspase-9 (2-fold) and expressions of key proteins in the intrinsic apoptosis pathway in HT-29 cells.
Overall, our results demonstrated QuCaNPs exhibits improved anti-cancer activity on HT-29 cells.
本研究旨在合成槲皮素-咖啡酸苯乙酯（CAPE）-共载聚乳酸-共-羟基乙酸（PLGA）纳米粒（QuCaNP），并研究其对人结肠直肠癌细胞 HT-29 的抗癌活性。
采用单乳液（o/w）溶剂蒸发法合成 QuCaNPs。测定 QuCaNPs 的粒径、Zeta 电位、多分散指数、释放曲线和表面形态。研究了 QuCaNPs 的细胞毒性、抗迁移、抗增殖和凋亡活性。
QuCaNP 的平均直径为 237.8±9.670nm，多分散指数（PDI）为 0.340±0.027。槲皮素的包封效率为 74.28%，CAPE 的包封效率为 65.24%。QuCaNP 在-20°C 下稳定 30 天，粒径和药物含量保持稳定。QuCaNP 处理 HT-29 细胞的半最大抑制浓度（IC）值分别为 11.2μg/mL（24 小时）和 8.2μg/mL（48 小时）。QuCaNP 处理可增加 HT-29 细胞中 caspase-3（2.38 倍）和 caspase-9（2 倍）的 mRNA 水平，并表达内在凋亡途径中的关键蛋白。
总的来说，我们的结果表明 QuCaNP 对 HT-29 细胞表现出增强的抗癌活性。
