State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China; Beijing Key Laboratory of Drug Delivery Technology and Novel Formulations, Department of Pharmaceutics, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China.
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China; Beijing Key Laboratory of Drug Delivery Technology and Novel Formulations, Department of Pharmaceutics, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China; Department of Pharmacy, Yanbian University, Yanji, Jilin 133000, PR China.
Food Chem. 2023 Aug 30;418:135939. doi: 10.1016/j.foodchem.2023.135939. Epub 2023 Mar 14.
Epigallocatechin gallate (EGCG) has attracted the increasing attention of many researchers, especially in the field of tumor therapy. However, EGCG has poor fat solubility, low stability, low bioavailability, and a high effective dose in vivo. Traditional drug delivery methods are difficult to deliver the water-soluble EGCG efficiently and in high doses to tumor sites. To address these issues, a new type of strategy has been tried in this study to transform EGCG from a "Bioactive natural ingredient" into a "Bioactive drug carrier". Briefly, the EGCG was modified with a fat-soluble 9-fluorene methoxy carbonyl (Fmoc) motif, and the obtained EGCG-Fmoc showed a considerable improvement in lipid solubility and stability. Interestingly, EGCG-Fmoc obtained the characteristic of self-assembly in water, making it easier to take up by tumor cells. Furthermore, the self-assembled nanocomplex exhibited paclitaxel encapsulation performance and could achieve the dual delivery of EGCG and paclitaxel.
没食子儿茶素没食子酸酯(EGCG)引起了许多研究人员的越来越多的关注,尤其是在肿瘤治疗领域。然而,EGCG 的脂溶性差、稳定性低、生物利用度低,体内有效剂量高。传统的药物输送方法难以将水溶性 EGCG 高效、高剂量地递送到肿瘤部位。为了解决这些问题,本研究尝试了一种新型策略,将 EGCG 从“生物活性天然成分”转变为“生物活性药物载体”。简而言之,用脂溶性 9-芴甲氧羰基(Fmoc)基修饰 EGCG,得到的 EGCG-Fmoc 显著提高了脂溶性和稳定性。有趣的是,EGCG-Fmoc 在水中具有自组装特性,使其更容易被肿瘤细胞摄取。此外,自组装纳米复合物具有紫杉醇包封性能,可以实现 EGCG 和紫杉醇的双重递药。