A brain tumour is an uncontrolled cell proliferation, forming a mass of tissue
composed of cells that grow and divide abnormally, seemingly beyond the control of
the body’s normal regulatory processes. Approximately 70% of primary malignant
brain tumors diagnosed each year originate from glial cells. The physiological bloodbrain barrier (BBB) impairs drug distribution to the tumour microenvironment and
complicates the treatment of malignant brain tumours. Most of the conventional
chemotherapeutics lack specificity and lead to serious systemic toxicity. However,
nanocarriers have shown efficient therapeutic efficacy in delivering medications to the
brain tumour cells. The targeting of nanocarriers to the tumour sites can be achieved by
active or passive targeting. The dimensions and the physicochemical properties of the
nanocarriers significantly affect brain permeability. Among various nanotools,
branched PAMAM, PPL, and PPI dendrimers possess great efficacy in transporting
chemotherapeutic agents across the BBB for treating brain tumours. This chapter
discusses the various generations of dendrimers, their synthesis techniques, and the
passive and active targeting strategies used to deliver chemotherapeutics to the tumour
sites. The chapter also includes dendrimers as diagnostics and contrast agents in brain
tumour diagnosis. Dendrimers have been established as remarkable in diagnosing and
treating brain tumours, as they can transport the therapeutically active agents across the
BBB to the cancer cells after systemic administration. Different dendrimers like
PAMAM, PLL, PPI, carbosilanes, and phosphorus-based are used to develop novel
therapeutics having prolonged and controlled drug release, immunotherapy, and
anticancer activity. This chapter can provide remarkable guidance to scientists working
on brain-targeting delivery systems.
Keywords: Brain tumour, Dendrimers, Imaging, Passive and active targeting, Therapeutics.
