School of Pharmaceutical Sciences, Southwest University, Chongqing, People's Republic of China.
Int J Nanomedicine. 2018 Mar 15;13:1601-1610. doi: 10.2147/IJN.S157019. eCollection 2018.
Glioma is the most aggressive and lethal brain tumor in humans, it comprises about 30 per cent of all brain tumors and central nervous system tumors.
The objective of this study was to create novel brain-targeting nanoliposomes to encapsulate curcumin as a promising option for glioma therapy.
Human glioma cells (U251MG) were used to determine cell uptake efficiency and possible internalization mechanism of the curcumin-loaded nanoliposomes modified by a brain-targeting peptide RDP. In addition, intracranial glioma mice model was prepared by transplantation of U251MG cells into the mice striatum, and then the liposomes were intravenously administered into the glioma-bearing mice to evaluate the anti-glioma activity.
RDP-modified liposomes (RCL) could enter the brain and glioma region, and were internalized by the glioma cells perhaps through acetylcholine receptor-mediated endocytosis pathway. Furthermore, the RCL prolonged the survival time of the glioma-bearing mice from 23 to 33 days, and the inhibition mechanism of the RCL on glioma cell was partly due to cell cycle arrest at the S phase and induction of cell apoptosis.
This study would provide a potential approach for targeted delivery of drug-loaded liposomes for glioma treatment.
脑胶质瘤是人类最具侵袭性和致命性的脑肿瘤，约占所有脑肿瘤和中枢神经系统肿瘤的 30%。
本研究旨在构建新型脑靶向纳米脂质体来包载姜黄素，以期为脑胶质瘤治疗提供新的选择。
用人脑胶质瘤细胞（U251MG）来确定载姜黄素的脑靶向肽 RDP 修饰的纳米脂质体的细胞摄取效率和可能的内化机制。此外，通过将 U251MG 细胞移植到小鼠纹状体来制备颅内脑胶质瘤小鼠模型，然后将脂质体经静脉给予脑胶质瘤荷瘤小鼠，以评估其抗脑胶质瘤活性。
RDP 修饰的脂质体（RCL）能够进入脑和脑肿瘤区域，并被脑胶质瘤细胞内化，可能通过乙酰胆碱受体介导的内吞作用途径。此外，RCL 延长了脑胶质瘤荷瘤小鼠的生存时间，从 23 天延长至 33 天，RCL 对脑胶质瘤细胞的抑制机制部分归因于 S 期细胞周期阻滞和诱导细胞凋亡。
本研究为脑靶向载药脂质体治疗脑胶质瘤提供了一种潜在的方法。
