Glioma, especially its most malignant type, Glioblastoma (GBM), is the most common
and the most aggressive malignant tumour in the central nervous system. Currently, we have no
specific therapies that can significantly improve its dismal prognosis. Recent studies have reported
promising in vitro experimental results of several novel glioma-targeting drugs; these studies are
encouraging to both researchers and patients. However, clinical trials have revealed that novel compounds
that focus on a single, clear glioma genetic alteration may not achieve a satisfactory outcome
or have side effects that are unbearable. Based on this consensus, phytochemicals that exhibit multiple
bioactivities have recently attracted much attention. Traditional Chinese medicine and traditional
Indian medicine (Ayurveda) have shown that phytocompounds inhibit glioma angiogenesis, cancer
stem cells and tumour proliferation; these results suggest a novel drug therapeutic strategy. However,
single phytocompounds or their direct usage may not reverse comprehensive malignancy due
to poor histological penetrability or relatively unsatisfactory in vivo efficiency. Recent research that
has employed temozolomide combination treatment and Nanoparticles (NPs) with phytocompounds
has revealed a powerful dual-target therapy and a high blood-brain barrier penetrability, which is
accompanied by low side effects and strong specific targeting. This review is focused on major phytocompounds
that have contributed to glioma-targeting treatment in recent years and their role in
drug resistance inhibition, as well as novel drug delivery systems for clinical strategies. Lastly, we
summarize a possible research strategy for the future.