Simple SummaryNanomaterials are one of the most promising discoveries of this millennium. Thanks to the widest range of applications, this field has spread to all scientific disciplines. As well, interest has significantly increased in the medical sector. Although there are many different families of nanoparticles, carbon-based nanoparticles have only recently come to light. An infinite number of nanoparticles of various shapes and sizes can be produced by taking advantage of the chemical bonding properties of carbon, which also allows for the modification of their chemical, thermal, and physical properties. This review examines the biomolecular aspects of the theoretical and practical challenges involved in creating nanoparticles with biological activity, identifying the benefits and drawbacks of each approach, and summarizing the most recent research on carbon-based nanoparticles conceptualized and developed to date. Although it is a very promising area of study, more pharmacokinetic and toxicological research is still required.AbstractMalignant gliomas are the most common primary brain tumors in adults up to an extent of 78% of all primary malignant brain tumors. However, total surgical resection is almost unachievable due to the considerable infiltrative ability of glial cells. The efficacy of current multimodal therapeutic strategies is, furthermore, limited by the lack of specific therapies against malignant cells, and, therefore, the prognosis of these in patients is still very unfavorable. The limitations of conventional therapies, which may result from inefficient delivery of the therapeutic or contrast agent to brain tumors, are major reasons for this unsolved clinical problem. The major problem in brain drug delivery is the presence of the blood–brain barrier, which limits the delivery of many chemotherapeutic agents. Nanoparticles, thanks to their chemical configuration, are able to go through the blood–brain barrier carrying drugs or genes targeted against gliomas. Carbon nanomaterials show distinct properties including electronic properties, a penetrating capability on the cell membrane, high drug-loading and pH-dependent therapeutic unloading capacities, thermal properties, a large surface area, and easy modification with molecules, which render them as suitable candidates for deliver drugs. In this review, we will focus on the potential effectiveness of the use of carbon nanomaterials in the treatment of malignant gliomas and discuss the current progress of in vitro and in vivo researches of carbon nanomaterials-based drug delivery to brain.