Chen Zhongqin, Xu Leilei, Gao Xudong, Wang Chunli, Li Ruilin, Xu Jun, Zhang Min, Panichayupakaranant Pharkphoom, Chen Haixia
Tianjin Key Laboratory for Modern Drug Delivery & High-Efficiency, School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, PR China.
Tianjin Agricultural University, Tianjin 300384, PR China; State Key Laboratory of Nutrition and Safety, Tianjin University of Science & Technology, Tianjin 300457, PR China.
Food Res Int. 2020 Nov;137:109674. doi: 10.1016/j.foodres.2020.109674. Epub 2020 Sep 17.
The nanoparticle systems could effectively overcome the drug delivery challenges of food bioactive compounds. In this study, a novel and effective multifunctional PEG modified CeO@SiO nanoparticle (CSP-NPs) system was successfully fabricated. Food derived proanthocyanidin (PAC) and curcumin (Cur) were loaded onto CSP-NPs and formed as PAC-NPs and Cur-NPs. Fourier transform Infrared spectra, X-ray diffraction, scanning electron microscopy, transmission electron microscopy, and dynamic light scattering were used to characterize the prepared NPs. CSP-NPs, PAC-NPs and Cur-NPs displayed spherical shape with about 35-45 nm size. The bioactivity analysis revealed that CSP-NPs system could effectively deliver PAC and Cur to exhibit strong antioxidant activity, potent neuroprotective effect against Aβ-mediated toxicity in PC-12 cells (recovered cell viability from 57.5% to 81.0% at the dose of 25 μg/mL) and effective antiproliferative effects on HepG2 and Hela cells. Besides, all prepared nanoparticles (0-100 µg/ml) used in this study showed no significant toxicity on cell models of antioxidative and neuroprotective activities, excepting for cancer cells, suggesting that these nanoparticles had the potential of being utilized in drug delivery. Therefore, CSP-NPs might be a promising delivery system for hydrophilic molecule proanthocyanidin and hydrophobic molecule curcumin against the oxidative damage, neurodegenerative diseases and cancer, which could facilitate the application of food derived nutrients in functional foods industry.
纳米颗粒系统能够有效克服食品生物活性化合物的药物递送挑战。在本研究中,成功制备了一种新型且有效的多功能聚乙二醇修饰的CeO@SiO纳米颗粒(CSP-NPs)系统。将食品来源的原花青素(PAC)和姜黄素(Cur)负载到CSP-NPs上,形成PAC-NPs和Cur-NPs。利用傅里叶变换红外光谱、X射线衍射、扫描电子显微镜、透射电子显微镜和动态光散射对制备的纳米颗粒进行表征。CSP-NPs、PAC-NPs和Cur-NPs呈球形,尺寸约为35-45纳米。生物活性分析表明,CSP-NPs系统能够有效递送PAC和Cur,表现出强大的抗氧化活性、对PC-12细胞中Aβ介导的毒性具有显著的神经保护作用(在25μg/mL剂量下,细胞活力从57.5%恢复到81.0%)以及对HepG2和Hela细胞有效的抗增殖作用。此外,本研究中使用的所有制备的纳米颗粒(0-100μg/ml)对抗氧化和神经保护活性的细胞模型均无明显毒性,但对癌细胞除外,这表明这些纳米颗粒具有用于药物递送的潜力。因此,CSP-NPs可能是一种有前景的递送系统,用于亲水性分子原花青素和疏水性分子姜黄素,以对抗氧化损伤、神经退行性疾病和癌症,这有助于食品来源的营养成分在功能性食品工业中的应用。