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Published on: March 28, 2021
Progress in research and development of temozolomide brain-targeted preparations: a review
Jiefen Yang1, Youfa Xu1,2, Zhiqin Fu1,2
1Department of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou, China.
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.
Insights
Nano-formulations enhance brain drug concentration for glioma treatment. These systems improve temozolomide (TMZ) efficacy and reduce side effects, offering new hope for patients with aggressive brain tumors.
Area of Science:
- Neuro-oncology
- Nanomedicine
- Drug Delivery Systems
Background:
- Gliomas are aggressive brain tumors with poor prognosis, often requiring surgical resection.
- Temozolomide (TMZ) is a key chemotherapy agent, but faces challenges like low efficacy and drug resistance.
- Systemic administration of TMZ can lead to adverse effects and limited brain drug concentration.
Approach:
- Review of various nano-formulations designed for targeted delivery of temozolomide (TMZ) to gliomas.
- Analysis of how nanotechnology overcomes limitations in TMZ penetration and enhances brain tumor targeting.
- Discussion of research progress in developing advanced drug delivery systems for glioma therapy.
Key Points:
- Nano-formulations significantly increase the concentration of temozolomide (TMZ) within the brain.
- These advanced delivery systems improve TMZ's anti-proliferative and cytotoxic effects against glioma cells.
- Nanotechnology-based approaches mitigate systemic toxicity and overcome drug resistance associated with TMZ.
Conclusions:
- Nano-formulations represent a promising strategy to enhance the clinical effectiveness of temozolomide (TMZ) for glioma treatment.
- Further research and development in drug delivery systems are crucial for optimizing glioma therapy.
- The reviewed data offers valuable insights for the clinical application of TMZ nano-formulations in managing gliomas.

