Glioblastoma is the most aggressive type of malignant brain tumour and is associated with a high mortality rate. Current standard therapy for glioblastoma is inadequate due to tumour resistance and recurrence. Recent efforts in producing targeted therapies for glioblastoma have also faced challenges due to the blood brain barrier and the tumour heterogeneity of glioblastomas. As a result, there is a need for novel treatment strategies. Triterpenoid derivatives are well known to possess a wide range of anti-cancer effects. With its multifaceted action, selective toxicity, chemosensitising effect and ability to penetrate the blood brain barrier, triterpenoids are believed to have a potential role in the treatment of glioblastoma. However, the limited aqueous solubility and non-specific bio-distribution of triterpenoid derivatives have been obstacles to its clinical application. An effective method for delivering triterpenoid derivatives has yet to be developed that would further elucidate the precise mechanism of triterpenoid derivatives in treating glioblastoma. We aimed to develop triterpenoid derivative micellar nanoparticles that would further elucidate the precise mechanism of triterpenoid derivatives in treating glioblastoma. Triterpenoid derivatives were synthesised into nanoparticles using micelles. The particle size, encapsulation efficiency, in vitro release, stability, cytotoxicity, and cellular uptake of these triterpenoid nanoparticles were characterised in human glioblastoma (U87MG) cells. Micellar nanoparticles significantly improve triterpenoid derivatives solubility, stability, and bioavailability in vitro (n = 3, P<0.05). Micellar nanoparticles significantly improve the anti-glioblastoma dose dependent inhibition of the triterpenoids compared to the standard chemotherapeutic agent, temozolomide (n = 3, P<0.05). We hypothesise that triterpenoid derivatives may be inhibiting the PI3K/Akt signalling pathway, which plays a major role in mediating the responses of glioblastoma cells to triterpenoid derivatives, and the potential use of triterpenoid derivatives in treating glioblastoma.