Introduction. Glioblastoma is the most aggressive type of brain cancer and the current standard chemotherapy temozolomide is inadequate due to tumour resistance and recurrence. Natural products including triterpenoids, have previously shown cytotoxicity against glioblastoma cells. However, their poor physiochemical properties, pharmacokinetics and pharmacodynamics have restricted their use in brain cancer patients.
Aims. In this study, different nanoformulations of natural products derivatives were prepared to improve their in vitro solubility and cytotoxicity.
Methods. The cytotoxicity of natural product nanoformulations alone or in combination against U87MG glioblastoma cells was evaluated using in vitro cell viability assays. The particle size and loading capacity of the fabricated nanoparticles were assessed by using dynamic light scattering and HPLC, respectively.
Results. The highly soluble nanoformulations were shown to enhance the cytotoxicity of natural products derivatives (p <0.05). Excitingly, the nanoformulations significantly lowered the dose (IC50) of glioblastoma chemotherapeutic temozolomide required in combination experiments (p <0.05).
Discussion. Natural product derivatives nanoformulations successfully improved the brain cancer in vitro cytotoxic activity. Brain cancer in vitro temozolomide sensitivity also improved when used in combination. This suggests that we could potentially combine the natural product derivatives nanoformulations with temozolomide in brain cancer patients. By utilising the increased sensitivity to temozolomide, we could reduce brain cancer resistance and recurrence, reduce the dose required (reduced side effects), thus improve brain cancer patient outcomes.