期刊
JOURNAL OF LIPOSOME RESEARCH
卷 29, 期 1, 页码 21-34出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/08982104.2017.1408649
关键词
RGD; vinorelbine; tetrandrine; blood-brain barrier; multidrug resistance
资金
- National Natural Science Foundation of China [81541081]
Brain glioma is one of the most common and devastating intracranial malignancies with a high mortality. Chemotherapy for brain glioma is not ideal due to blood brain barrier (BBB) and multidrug resistance (MDR). The objectives of the present study were to develop a kind of RGD (Arg-Gly-Asp) tripeptide modified vinorelbine plus tetrandrine liposomes to achieve BBB transportation, MDR reversion and glioma cell targeting simultaneously. The studies were performed on glioma cells, resistant glioma cells and glioma-bearing mice. Results showed that the constructed liposomes with suitable physicochemical properties could significantly enhance the transport across BBB, obviously accumulate in glioma cells, and exhibit evident capabilities in diminishing brain glioma in mice. Action mechanism studies indicated that the enhanced anticancer efficacy could be attribute to the follows: prolonged elimination half-life (7.093 +/- 1.311h); increased AUC(0-24h) (28.92 +/- 2.66mg/L*h); transporting across BBB; enhanced cellular uptake; down-regulation on P-gp (0.49 +/- 0.06 fold); inducing apoptosis via activating caspase 8, 9, and 3 (2.40 +/- 0.22, 3.57 +/- 0.29, and 4.33 +/- 0.30 folds, respectively). In conclusion, the RGD modified vinorelbine plus tetrandrine liposomes may offer a promising therapeutic strategy for treatment of brain glioma.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据