Progress in research and development of temozolomide brain-targeted preparations: a review.

Gliomas are a heterogeneous group of brain tumours with high malignancy, for which surgical resection remains the mainstay of treatment at present. However, the overall prognosis of gliomas remains poor because of their aggressiveness and high recurrence. Temozolomide (TMZ) has anti-proliferative and cytotoxic effects and is indicated for glioblastoma multiforme and recurrent mesenchymal astrocytoma. However, TMZ is disadvantaged by low efficacy and drug resistance, and therefore it is necessary to enhance the brain drug concentration of TMZ to improve its effectiveness and reduce the toxic and adverse effects from systemic administration. There have been many nano-formulations developed for the delivery of TMZ to gliomas that overcome the limitations of TMZ penetration to tumours and increase brain targeting. In this paper, we review the research progress of TMZ nano-formulations, and also discuss challenges and opportunities in the research and development of drug delivery systems, hoping that the data and information summarised herein could provide assistance for the clinical treatment of gliomas.