Department of Pharmaceutical Sciences, North South University, Dhaka 1229, Bangladesh.
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Molecules. 2020 Nov 20;25(22):5453. doi: 10.3390/molecules25225453.
Inflammation is responsible for the development of many diseases that make up a significant cause of death. The purpose of the study was to develop a novel nanophytosomal preparation of epigallocatechin-3-gallate (EGCG) and egg phospholipid complex that has a lower particle size with higher drug loading capability, physical stability and anti-inflammatory activities. The impact of different factors and material characteristics on the average particle size was studied along with the drug loading of phytosome using design of experiment (DoE). The in vivo anti-inflammatory study was evaluated using a rat model to investigate the performance of EGCG nanophytosome. UHPLC results showed that 500 µg of EGCG were present in 1 mL of green tea extract. SEM data exhibited that phytosome (phospholipid-drug complex) was in the nanosize range, which was further evident from TEM data. Malvern Zetasizer data showed that the average particle size of the EGCG nanophytosome was in the range of 100-250 nm. High drug loading (up to 90%) was achieved with optimum addition rate, stirring temperature and phospholipid concentration. Stability study data suggest that no significant changes were observed in average particle size and drug loading of nanophytome. The in vivo anti-inflammatory study indicated a significant anti-inflammatory activity of green tea extract, pure EGCG and its phytosomal preparations ( ≤ 0.001) against acute paw edema.
炎症是许多疾病发展的原因，这些疾病是导致死亡的重要原因。本研究的目的是开发一种新型的表没食子儿茶素没食子酸酯（EGCG）和卵磷酯复合物纳米植物药，该药物具有更小的粒径、更高的载药量、更好的物理稳定性和抗炎活性。本研究通过实验设计（DoE）研究了不同因素和材料特性对平均粒径和载药量的影响。通过大鼠模型评估了体内抗炎研究，以考察 EGCG 纳米植物药的性能。UHPLC 结果表明，1 毫升绿茶提取物中含有 500 µg 的 EGCG。SEM 数据显示，植物药（磷脂-药物复合物）处于纳米尺寸范围内，这从 TEM 数据中进一步得到证实。马尔文 Zetasizer 数据显示，EGCG 纳米植物药的平均粒径在 100-250nm 范围内。通过最佳添加率、搅拌温度和磷脂浓度，实现了高达 90%的高载药量。稳定性研究数据表明，纳米植物药的平均粒径和载药量没有明显变化。体内抗炎研究表明，绿茶提取物、纯 EGCG 及其植物药制剂（≤0.001）对急性爪肿胀具有显著的抗炎活性。
