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Multifunctional liposomes loaded with paclitaxel and artemether for treatment of invasive brain glioma
Xiu-Ying Li1, Yao Zhao1, Meng-Ge Sun1
1State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
Abstract:
Invasive brain glioma is the most lethal type of cancer and is highly infiltrating. This leads to an extremely poor prognosis and makes complete surgical removal of the tumor virtually impossible. Non-penetration of therapeutic drugs across the blood-brain barrier (BBB), brain cancer stem cells (CSCs), and brain cancer vasculogenic mimicry (VM) results in relapse after surgical and radio therapy. We developed a functional targeting chemotherapy for transporting drugs across the BBB, destroying VM channels, and eliminating CSCs and cancer cells in the brain. The studies were undertaken on brain glioma cells in vitro and in brain glioma-bearing rats. Using paclitaxel as the anticancer drug and artemether as the regulator of apoptosis and inhibitor of VM channels, a kind of functional targeting paclitaxel plus artemether liposomes was developed by modifying two new functional materials: a mannose-vitamin E derivative conjugate (MAN-TPGS1000) and a dequalinium-lipid derivative conjugate (DQA-PEG2000-DSPE). The transport mechanism across the BBB was associated with receptor-mediated endocytosis by MAN-TPGS1000 conjugate via glucose transporters and adsorptive-mediated endocytosis by DQA-PEG2000-DSPE conjugate via electric charge-based interactions. The efficacy was related to the destruction of VM channels by regulating VM indicators, as well as the induction of apoptosis in brain cancer cells and CSCs by activating apoptotic enzymes and pro-apoptotic proteins and inhibiting anti-apoptotic proteins. These data suggest that the chemotherapy using functional targeting paclitaxel plus artemether liposomes could provide a new strategy for treating invasive brain glioma.
Insights
A novel liposome therapy effectively delivers chemotherapy across the blood-brain barrier to target brain glioma, destroying vasculogenic mimicry and eliminating cancer stem cells for improved treatment outcomes.
Area of Science:
- Neuro-oncology
- Nanomedicine
- Drug Delivery
Background:
- Invasive brain glioma presents a poor prognosis due to its infiltrating nature and challenges in complete surgical removal.
- Therapeutic drug delivery is hindered by the blood-brain barrier (BBB), brain cancer stem cells (CSCs), and vasculogenic mimicry (VM), leading to treatment relapse.
Purpose of the Study:
- To develop a functional targeting chemotherapy to overcome BBB penetration, destroy VM channels, and eliminate CSCs and glioma cells.
- To investigate the efficacy of paclitaxel and artemether loaded into functionalized liposomes in vitro and in vivo.
Main Methods:
- Development of functional targeting liposomes encapsulating paclitaxel and artemether, modified with MAN-TPGS1000 and DQA-PEG2000-DSPE conjugates.
- Investigation of BBB transport mechanisms via receptor-mediated and adsorptive-mediated endocytosis.
- Assessment of anti-cancer efficacy through VM channel destruction and induction of apoptosis in glioma cells and CSCs.
Main Results:
- The functional targeting liposomes demonstrated effective transport across the BBB through specific endocytosis pathways.
- The chemotherapy induced apoptosis in brain cancer cells and CSCs by modulating apoptotic proteins.
- The treatment successfully destroyed VM channels, a key factor in glioma progression and relapse.
Conclusions:
- Functional targeting liposomes loaded with paclitaxel and artemether offer a promising new strategy for invasive brain glioma treatment.
- This approach addresses critical challenges including BBB penetration, CSCs, and VM, potentially improving patient outcomes.
