文献类型：期刊文献

英文题名：Intravenous delivery of enzalutamide based on high drug loading multifunctional graphene oxide nanoparticles for castration-resistant prostate cancer therapy

作者：Jiang, Wenjun[1,2];Chen, Jiyuan[1];Gong, Chunai[3];Wang, Yuanyuan[1];Gao, Yuan[1,4];Yuan, Yongfang[3]

机构：[1]Fudan Univ, Sch Pharm, Dept Clin Pharm & Pharmaceut Management, 826 Zhangheng Rd, Shanghai 201203, Peoples R China;[2]East China Univ Sci & Technol, Dept Pharm, 130 Meilong Rd, Shanghai 200237, Peoples R China;[3]Shanghai Jiao Tong Univ, Sch Med, Shanghai Peoples Hosp 9, Dept Pharm, 639 Zhizaoju Rd, Shanghai 200011, Peoples R China;[4]Second Mil Med Univ, Changhai Hosp, Dept Pharm, 168 Changhai Rd, Shanghai 200433, Peoples R China

年份：2020

卷号：18

期号：1

外文期刊名：JOURNAL OF NANOBIOTECHNOLOGY

收录：;EI(收录号：20201608427536);WOS:【SCI-EXPANDED(收录号:WOS:000522085700001)】；

基金：This work was supported by the National Natural Science Foundation of China (Grant Numbers 81672545, 81972392, and 81973275) and Shanghai Municipal Health Commission (201840306).

语种：英文

外文关键词：Redox-sensitive; Enzalutamide; Graphene quantum dot derivate; Castration-resistant prostate cancer

摘要：Background Enzalutamide (Enz) has shown limited bioavailability via oral administration. Castration-resistant prostate cancer (CRPC) is frequent among patients receiving 18-24 months of androgen deprivation therapy. The nonsteroidal anti-androgen enzalutamide (Enz) used in the treatment of prostate cancer has shown limited bioavailability via oral administration. Therefore, we developed a multifunctional enzalutamide-loaded graphene oxide nanosystem (TP-GQDss/Enz) for CRPC intravenous treatment, with high drug loading efficiency. Methods Aminated graphene quantum dots (GQDs) were first cross-linked via disulfide bonds into a graphene quantum dot derivative of approximately 200 nm (GQDss), which was further functionalized with a tumour-targeting peptide and PEG to form TP-GQDss. Enz was loaded into TP-GQDss for in vitro and in vivo study. Results The results showed that high drug-loading efficiency was achieved by TP-GQDss via pi-pi electron interaction. TP-GQDss could be rapidly internalized by CRPC cells via endocytosis. Moreover, Enz in TP-GQDss could inhibit the growth of C4-2B and LNCaP prostate cancer cell lines in vitro. Further, TP-GQDss exhibited an enhanced cancer-targeting ability and alleviated the side effects of Enz in vivo. Conclusions The multifunctional nanocarrier constructed here could accomplish controlled Enz release and serve as an intravenous therapy platform for CRPC.