School of Pharmacy and Health Professionals, Creighton University, Omaha, Nebraska, 68178, USA.
College of Saint Mary, Omaha, Nebraska, USA.
AAPS PharmSciTech. 2019 Apr 15;20(5):163. doi: 10.1208/s12249-019-1379-y.
Cataract, one of the leading causes of blindness worldwide, is a condition in which complete or partial opacity develops in the lens of the eyes, thereby impairing vision. This study aimed to examine the potential therapeutic and protective effects of poorly soluble polyphenols like curcumin, resveratrol, and dibenzoylmethane, known to possess significant antioxidant activity. The polyphenols were loaded into novel lipid-cyclodextrin-based nanoparticles and characterized by particle size, polydispersity index, differential scanning calorimetry, thermogravimetric analysis, X-ray diffraction, scanning electron microscopy (SEM), entrapment efficiency, and release studies. Ferric-reducing ability of plasma and 2,2-diphenyl-1-picrylhydrazyl chemical assays were used to evaluate their antioxidant properties based on their free radical quenching ability. Biochemical in vitro assays were used to examine these polyphenols on hydrogen peroxide-induced formation of cataracts in bovine lenses by estimating total glutathione content and superoxide dismutase activity. Nanoparticles were thermostable and amorphous. Particle size of curcumin, resveratrol, and dibenzoylmethane nanoparticles were 331.0 ± 17.9 nm, 329.9 ± 1.9 nm, and 163.8 ± 3.2 nm, respectively. SEM confirmed porous morphology and XRD confirmed physical stability. Entrapment efficiency for curcumin-, resveratrol-, and dibenzoylmethane-loaded nanoparticles was calculated to be 84.4 ± 2.4%, 72.2 ± 1.5%, and 86.4 ± 0.6%, respectively. In vitro release studies showed an initial burst release followed by a continuous release of polyphenols from nanoparticles. Chemical assays confirmed the polyphenols' antioxidant activity. Superoxide dismutase and glutathione levels were found to be significantly increased (p < 0.05) after treatment with polyphenol-loaded nanoparticles than pure polyphenols; thus, an improved antioxidant activity translational into potential anticataract activity of the polyphenols when loaded into nanoparticles was observed as compared to pure polyphenols.
白内障是全球致盲的主要原因之一，是眼睛晶状体完全或部分不透明的一种病症，从而损害视力。本研究旨在研究难溶性多酚（如姜黄素、白藜芦醇和二苯甲酰甲烷）的潜在治疗和保护作用，这些多酚具有显著的抗氧化活性。多酚被负载到新型的脂质-环糊精纳米粒子中，并通过粒径、多分散指数、差示扫描量热法、热重分析、X 射线衍射、扫描电子显微镜（SEM）、包封效率和释放研究进行了表征。基于其自由基猝灭能力，使用铁还原能力的血浆和 2,2-二苯基-1-苦基肼化学测定法来评估它们的抗氧化性能。通过估计总谷胱甘肽含量和超氧化物歧化酶活性，在体外生物化学测定中研究了这些多酚对牛晶状体中过氧化氢诱导白内障形成的影响。纳米粒子热稳定且无定形。姜黄素、白藜芦醇和二苯甲酰甲烷纳米粒子的粒径分别为 331.0±17.9nm、329.9±1.9nm 和 163.8±3.2nm。SEM 证实了多孔形态，XRD 证实了物理稳定性。姜黄素、白藜芦醇和二苯甲酰甲烷负载纳米粒子的包封效率分别计算为 84.4±2.4%、72.2±1.5%和 86.4±0.6%。体外释放研究表明，纳米粒子中多酚的释放呈现初始突释，随后是持续释放。化学测定证实了多酚的抗氧化活性。与单独使用多酚相比，用负载多酚的纳米粒子处理后，超氧化物歧化酶和谷胱甘肽水平显著升高（p<0.05）；因此，与单独使用多酚相比，将多酚负载到纳米粒子中可提高抗氧化活性，从而观察到多酚具有潜在的抗白内障活性。
