Wiggers Heliton Augusto, Fin Margani Taise, Khalil Najeh Maissar, Mainardes Rubiana Mara
Pharmaceutical Nanotechnology Laboratory, Department of Pharmacy, Midwest State University, Alameda Élio Antonio Dalla Vecchia St, 838, 85040-167 Guarapuava, PR, Brazil.
Food Technol Biotechnol. 2022 Jun;60(2):145-154. doi: 10.17113/ftb.60.02.22.6981.
Gallic acid is a polyphenol with antioxidant and antitumor activities; however, its use as a nutraceutical or drug is hindered by its low bioavailability. Zein is a natural protein found in corn and has been applied as nanoparticle drug carrier. In this study, zein nanoparticles were obtained and stabilized with polyethylene glycol (PEG) as gallic acid carriers.
Nanoparticles were obtained by the liquid-liquid method and characterized in terms of mean size, polydispersity index, zeta potential, morphology, solid-state interactions and encapsulation efficiency/drug loading. The stability of nanoparticles was evaluated in simulated gastrointestinal fluids and food simulants, and the antioxidant activity was determined by the scavenging of the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical.
Zein nanoparticles containing gallic acid were obtained and stabilized only in the presence of PEG. Under optimal conditions, nanoparticles with mean size <200 nm, low polydispersity index (<0.25) and negative zeta potential (-20 mV) were obtained. The gallic acid encapsulation efficiency was about 40%, loading about 5%, and it was encapsulated in an amorphous state. Fourier transform infrared spectroscopy (FTIR) did not identify chemical interactions after gallic acid nanoencapsulation. Zein nanoparticles were more prone to release the gallic acid in gastric than intestinal simulated medium; however, more than 50% of drug content was protected from premature release. In food simulants, the gallic acid release from nanoparticles was prolonged and sustained. Moreover, the nanoencapsulation did not reduce the antioxidant activity of gallic acid.
The results show the importance of PEG in the formation and its effect on the properties of zein nanoparticles obtained by the liquid-liquid dispersion method. This study indicates that PEG-stabilized zein nanoparticles are potential carriers for oral intake of gallic acid, preserving its antioxidant properties and enabling its use in the pharmaceutical and food industries.
没食子酸是一种具有抗氧化和抗肿瘤活性的多酚；然而，其作为营养保健品或药物的应用受到其低生物利用度的阻碍。玉米醇溶蛋白是一种存在于玉米中的天然蛋白质，已被用作纳米颗粒药物载体。在本研究中，制备了玉米醇溶蛋白纳米颗粒并用聚乙二醇（PEG）作为没食子酸载体进行稳定化处理。
通过液 - 液法制备纳米颗粒，并对其平均粒径、多分散指数、zeta电位、形态、固态相互作用以及包封效率/载药量进行表征。在模拟胃肠液和食品模拟物中评估纳米颗粒的稳定性，并通过2,2 - 二苯基 - 1 - 苦基肼（DPPH）自由基清除法测定抗氧化活性。
制备得到了含有没食子酸的玉米醇溶蛋白纳米颗粒，且仅在PEG存在下得以稳定。在最佳条件下，获得了平均粒径<200 nm、低多分散指数（<0.25）和负zeta电位（-20 mV）的纳米颗粒。没食子酸的包封效率约为40%，载药量约为5%，且以无定形状态被包封。傅里叶变换红外光谱（FTIR）在没食子酸纳米包封后未发现化学相互作用。玉米醇溶蛋白纳米颗粒在模拟胃液中比在模拟肠液中更容易释放没食子酸；然而，超过50%的药物含量可防止过早释放。在食品模拟物中，则延长并持续了纳米颗粒中没食子酸的释放。此外，纳米包封并未降低没食子酸的抗氧化活性。
结果表明PEG在通过液 - 液分散法获得的玉米醇溶蛋白纳米颗粒的形成过程中的重要性及其对颗粒性质的影响。本研究表明，PEG稳定的玉米醇溶蛋白纳米颗粒是口服没食子酸的潜在载体，可保留其抗氧化特性，并使其能够应用于制药和食品工业。
