In vitro and in vivo evaluation of functionalized chitosan–Pluronic micelles loaded with myricetin on glioblastoma cancer

This study aimed to develop a novel polymeric carrier based on chitosan-functionalized Pluronic P123/F68 micelles loaded with myricetin (MYR) to improve the therapeutic index of chemotherapy for glioblastoma cancer. Following characterization and assessment of the cellular uptake and antitumor effects of MYR-loaded micelles (MYR-MCs) in vitro, the acute toxicity, blood–brain barrier (BBB) translocation, brain uptake and biodistribution in vivo were assessed. The results demonstrated that MYR-MCs exhibited improved cellular uptake and antitumor activity compared to free MYR in vitro, with a significantly enhanced anticancer effect in vivo following efficient transport across the BBB. However, MYR-MCs did not affect the brain endothelial, barrier function, the liver, heart or kidneys. Furthermore, MYR-MCs altered the expression of apoptotic proteins, such as Bcl-2, BAD and BAX, in mice. In conclusion, MYR-MCs may be considered an effective and promising drug delivery system for glioblastoma treatment.

This study aimed to develop novel myricetin-loaded mixed micelles (MYR-MCs) for treating glioblastoma cancer. The enhanced anticancer effect that induced by MYR -MCs according to enhance the cellular uptake of MYR in Caco-2 cells and increase transport across an in vitro BBB layer. MYR-MCs treatments led to greater tumor remission and faster onset of antitumor activity and promoted apoptosis in vitro and in vivo, without detrimental effects on the brain endothelial or barrier function, the liver, heart or kidneys. Therefore, MYR-MCs seem to be an active and tolerable chemotherapy for glioblastoma cancer treatment.Figure optionsDownload high-quality image (125 K)Download as PowerPoint slide