Abstract
Surgery and radiotherapy cannot fully remove brain glioma; thus, chemotherapy continues to play an important role in treatment of this illness. However, because of the restriction of the blood-brain barrier (BBB) and the regeneration of glioma stem cells, post-chemotherapy relapse usually occurs. Here, we report a potential solution to these issues that involves a type of novel multifunctional vinblastine liposomes equipped with transferrin receptor binding peptide TfR-T12 and octa-arginine conjugate stearyl-R8. Studies were performed on brain glioma and glioma stem cells in vitro and were verified in brain glioma-bearing mice. The liposomes were transported across the BBB, killing brain glioma and glioma stem cells via the induction of necrosis, apoptosis and autophagy. Furthermore, we reveal the molecular mechanisms for treating brain glioma and glioma stem cells via functionalized drug lipid vesicles.
Highlights
Brain glioma is the most frequent primary malignant brain tumor, and the mean survival time of patients with this illness is only one year[1, 2]
The PEG2000-DSPE component of transferrin receptors (TfRs)-T12-PEG2000-DSPE and the stearyl component of stearyl-R8 were inserted into the lipophilic bilayer; the TfR-T12 and R8 components were left on the liposome exterior as the functional groups
The results showed that multifunctional vinblastine liposomes most strongly induced apoptosis effects in both brain glioma cells and glioma stem cells compared to the control groups
Summary
Brain glioma is the most frequent primary malignant brain tumor, and the mean survival time of patients with this illness is only one year[1, 2]. We propose a type of functionalized lipid vesicles, named as multifunctional vinblastine liposomes, which potentially transfer vinblastine across the BBB and subsequently eliminate brain glioma cells and glioma stem cells when equipped with the transferrin receptor binding peptide TfR-T12 and octa-arginine conjugate stearyl-R8. On brain glioma cells and glioma stem cells; these cells are rich in negative charges because of their increased activity compared to that of normal cells[9] These features can be used both to facilitate the transcytosis of functionalized drug carriers across the BBB and to potentiate the endocytosis of the carriers by brain glioma cells and glioma stem cells. Vinblastine is effective in killing brain glioma cells in vitro, it is ineffective in clinical chemotherapy because of the restriction of the BBB.
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