Pharmaceutical Nanotechnology Laboratory, Universidade Estadual do Centro-Oeste, Guarapuava, PR, Brazil; Chemistry Department, Universidade Tecnológica Federal do Paraná, Medianeira, PR, Brazil.
ICBAS - Institute of Biomedical Sciences Abel Salazar, University of Porto, Porto, Portugal; INEB - National Institute of Biomedical Engineering, University of Porto, Porto, Portugal; i3S - Institute for Research and Innovation in Health, University of Porto, Porto, Portugal.
Int J Biol Macromol. 2019 Oct 1;138:244-251. doi: 10.1016/j.ijbiomac.2019.07.030. Epub 2019 Jul 4.
The objective of this study was to develop zein-casein-lysine nanoparticles to modulate the intestinal permeability of ferulic acid (FA), a bioactive compound with proven antioxidant properties. The nanoparticles were obtained by a liquid-liquid dispersion method and were characterized in terms of mean size, polydispersity index, zeta potential, association efficiency (AE), in vitro drug release, x-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FT-IR). The in vitro intestinal permeability of nanoparticles was evaluated through Caco-2 and Caco-2/HT29-MTX monoculture and co-culture models, respectively. Nanoparticles presented a mean size of 199 nm and zeta potential of -26 mV. The AE of FA was 23% evaluated by high-performance liquid chromatography (HPLC). XRD showed amorphization of FA after association and FT-IR showed no changes in chemical structures of the compounds after nanoencapsulation. The cytotoxicity assays demonstrated that multicomposite nanoparticles presented a safe profile against Caco-2 and HT29-MTX cells. In the in vitro permeability assay, free FA exhibited higher permeability compared to FA-loaded nanoparticles, possibly due to prolonged FA release from nanoparticles. These new developed zein-casein-lysine nanoparticles may be used for FA sustained delivery by the oral route.
本研究旨在开发玉米醇溶蛋白-酪蛋白-赖氨酸纳米粒，以调节具有抗氧化性能的生物活性化合物阿魏酸（FA）的肠道通透性。纳米粒通过液-液分散法获得，并在粒径、多分散指数、Zeta 电位、结合效率（AE）、体外药物释放、X 射线衍射（XRD）和傅里叶变换红外光谱（FT-IR）等方面进行了表征。通过 Caco-2 和 Caco-2/HT29-MTX 单层和共培养模型分别评估了纳米粒的体外肠道通透性。纳米粒的平均粒径为 199nm，Zeta 电位为-26mV。通过高效液相色谱（HPLC）评估，FA 的 AE 为 23%。XRD 显示 FA 在结合后发生无定形化，FT-IR 显示纳米包封后化合物的化学结构没有变化。细胞毒性试验表明，多复合材料纳米粒对 Caco-2 和 HT29-MTX 细胞具有安全特性。在体外通透性试验中，与负载 FA 的纳米粒相比，游离 FA 表现出更高的通透性，这可能是由于纳米粒中 FA 的释放时间延长。这些新开发的玉米醇溶蛋白-酪蛋白-赖氨酸纳米粒可用于 FA 的口服缓释。
