Safwat Mohamed A, Kandil Bothaina A, Elblbesy Mohamed A, Soliman Ghareb M, Eleraky Nermin E
Department of Pharmaceutics, Faculty of Pharmacy, South Valley University, Qena 83523, Egypt.
Department of Radiological Science and Medical Imaging, Faculty of Allied Medical Science, Pharos University, Alexandria 21311, Egypt.
Pharmaceuticals (Basel). 2020 Sep 18;13(9):254. doi: 10.3390/ph13090254.
Epigallocatechin-3-gallate (EGCG) is a pleiotropic compound with anticancer, anti-inflammatory, and antioxidant properties. To enhance EGCG anticancer efficacy, it was loaded onto gold nanoparticles (GNPs). EGCG-GNPs were prepared by a simple green synthesis method and were evaluated using different techniques. Hemocompatibility with human blood and in vivo anticancer efficacy in Ehrlich ascites carcinoma-bearing mice were evaluated. EGCG/gold chloride molar ratio had a marked effect on the formation and properties of EGCG-GNPs where well-dispersed spherical nanoparticles were obtained at a molar ratio not more than 0.8:1. The particle size ranged from ~26 to 610 nm. High drug encapsulation efficiency and loading capacity of ~93 and 32%, respectively were obtained. When stored at 4 °C for three months, EGCG-GNPs maintained over 90% of their drug payload and had small changes in their size and zeta potential. They were non-hemolytic and had no deleterious effects on partial thromboplastin time, prothrombin time, and complement protein C3 concentration. EGCG-GNPs had significantly better in vivo anticancer efficacy compared with pristine EGCG as evidenced by smaller tumor volume and weight and higher mice body weight. These results confirm that EGCG-GNPs could serve as an efficient delivery system for EGCG with a good potential to enhance its anticancer efficacy.
表没食子儿茶素-3-没食子酸酯（EGCG）是一种具有抗癌、抗炎和抗氧化特性的多效化合物。为提高EGCG的抗癌疗效，将其负载于金纳米颗粒（GNPs）上。采用简单的绿色合成方法制备了EGCG-GNPs，并使用不同技术对其进行了评估。评估了其与人血的血液相容性以及在荷艾氏腹水癌小鼠体内的抗癌疗效。EGCG/氯化金摩尔比对EGCG-GNPs的形成和性质有显著影响，在摩尔比不超过0.8:1时可获得分散良好的球形纳米颗粒。粒径范围约为26至610nm。分别获得了约93%和32%的高药物包封率和载药量。当在4℃下储存三个月时，EGCG-GNPs保持了超过90%的药物负载量，其尺寸和zeta电位变化很小。它们无溶血作用，对部分凝血活酶时间、凝血酶原时间和补体蛋白C3浓度无有害影响。与原始EGCG相比，EGCG-GNPs在体内具有显著更好的抗癌疗效，表现为肿瘤体积和重量更小以及小鼠体重更高。这些结果证实，EGCG-GNPs可作为EGCG的有效递送系统，具有增强其抗癌疗效的良好潜力。
