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Penetration of blood–brain barrier and antitumor activity and nerve repair in glioma by doxorubicin-loaded monosialoganglioside micelles system

Lookup NU author(s): Ying Yin, Dr Jinju Chen, Dr Tieying Yin, Dr Yazhou Wang



This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License (CC BY-NC 4.0).


For the treatment of glioma and other central nervous system diseases, the one of the biggest challenges is that most therapeutic drugs cannot be delivered to the brain tumor tissue due to the blood-brain barrier. The goal of this manuscript is to construct a nanodelivery vehicle system with capabilities to overcome the blood-brain barrier for central nervous system administration. Doxorubicin as a model drug encapsulated in ganglioside GM1 micelles was able to achieve up to 9.33% loading efficiency and 97.05% encapsulation efficiency by orthogonal experimental design. The in vitro study demonstrated a slow and sustainable drug release in physiological conditions. In the cellular uptake studies, mixed micelles could effectively transport into both human umbilical vein endothelial cells and C6 cells. Furthermore, biodistribution imaging of mice showed that the DiR /GM1 mixed micelles were accumulated sustainably and distributed centrally in the brain. Experiments on zebrafish confirmed that drug-loaded GM1 micelles can overcome the blood-brain barrier and enter the brain. Among all the treatment groups, the median survival time of C6 bearing rats after administering DOX/GM1 micelles was significantly prolonged. In conclusion, the ganglioside nano micelles developed in this work can not only penetrate BBB effectively, but also can repair nerves and kill tumor cells at the same time.

Publication metadata

Author(s): Zou D, Wang W, Lei D, Yin Y, Ren P, Chen J, Yin T, Wang B, Wang G, Wang Y

Publication type: Article

Publication status: Published

Journal: International Journal of Nanomedicine

Year: 2017

Volume: 12

Pages: 4879-4889

Online publication date: 07/07/2017

Acceptance date: 07/06/2017

Date deposited: 18/07/2017

ISSN (print): 1176-9114

ISSN (electronic): 1178-2013

Publisher: Dove Medical Press Ltd.


DOI: 10.2147/IJN.S138257


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