胶质瘤
转铁蛋白受体
长春新碱
血脑屏障
脂质体
体内
药理学
药物输送
靶向给药
癌症研究
细胞毒性
脑瘤
靶向治疗
转铁蛋白
医学
体外
化疗
化学
生物
癌症
药品
病理
内科学
生物化学
中枢神经系统
环磷酰胺
有机化学
生物技术
作者
Solmaz Mojarad-Jabali,Masoud Farshbaf,Salar Hemmati,Muhammad Sarfraz,Hamidreza Motasadizadeh,Javid Shahbazi Mojarrad,Fatemeh Atyabi,Parvin Zakeri‐Milani,Hadi Valizadeh
标识
DOI:10.1016/j.ijpharm.2021.121395
摘要
The existence of the blood-brain barrier (BBB) makes the clinical chemotherapy of glioma a formidable challenge, because it hinders the passage of different chemotherapeutics into the brain and reduces the overall therapeutic efficiency. Therefore, it is necessary to design a drug delivery system in way that would favor the transportation of anti-cancer agents across the BBB and increase their selective accumulation within the tumor cells without affecting the normal tissues. Transferrin receptor (TfR) that shows an elevated level of expression on the BBB and glioma cells emerges as a promising tool for brain targeted delivery and glioma therapy. However, only a limited number of studies have comparatively evaluated the functionally of TfR targeting ligands. Herein, a series of liposomal formulations modified with the most well-known TfR targeting peptides including T12 (also known as THR), B6, and T7 was developed and their brain targeting capability and selective glioma accumulation was comparatively evaluated in vitro and in vivo. Among all TfR targeting or non-targeting groups, T7-modified liposomes (T7-LS) showed the highest BBB penetration capacity and brain distribution and displayed an enhanced accumulation in glioma cells. When loaded with vincristine (VCR), as a model chemotherapeutic, T7-LS/VCR could achieve the best anti-glioma outcome by means of targeted cytotoxicity and apoptosis in vitro. The obtained results suggested T7-LS as a potential platform for effective brain targeted delivery and glioma therapy in clinic.
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