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

Abstract

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.

Keywords:

• Temozolomide
• glioma
• nanoparticles
• brain targeting

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This study was supported by the National Natural Science Foundation of China (Nos. 81772749, 81872220, China); Shanghai Sailing Program (20YF1412100, China); Jiaxing Key Laboratory of Oncological Photodynamic Therapy and Targeted Drug Research as the basic public welfare research project of Zhejiang Province (No. LGF18H160034, China); The New Interdisciplinary Subjects of Pudong New District Health Committee, grant number (PWXx2020-04, China); Shanghai Qingpu District Industry-University-Research Cooperative Development Funding Project (2021-7, China), Program of Shanghai Academic Research Leader (21XD1403400, China), Nature Science Foundation of Shanghai (21ZR1449200, China) and High-level Talents of Fujian University of Chinese Medicine (X2019006-Talents, China).