The brain, administrator of the whole body is a delicate and soft organ of the body that controls and regulates most of our abilities to think, see, feel, hear, and much more. The administrator has very tight security unlike other organs called the blood-brain barrier (BBB) which allows only limited things to enter the brain. The protection (BBB) is full of a series of defences that helps to protect the brain from most of the internal and external threats. The presence of these protections, most importantly BBB, also offers difficulties to treat any disease condition in the brain. But, the advancement in neuroscience and drug delivery research has accorded many possible ways to bypass, open, or cross this barrier to treat brain diseases effectively including cancer. BBB is provided with a layer of endothelial cells which also cover the outer layer of all other organs and blood vessels in the body. Generally, this endothelial cell layer has gaps to allow passage of different important materials including nutrients and medicines through the layer. But, in the case of brain, these gaps are covered and blocked with proteins that restrict and controls the passage of materials through the layer. For example, necessary items like glucose, insulin and oxygen are allowed while toxins, bacteria and most of medicines are not allowed. Brain cancer is a rapidly expanding disease affecting a large population and is the 10th dominant cause of mortality. The survival rate for brain cancer patients after starting the treatment with radiation and chemotherapy is less than a year. Treatment of brain cancer with chemotherapeutics is very limited due to the presence of BBB and therefore their restricted entry to the brain. Strategies acquired to deliver chemotherapeutic drugs to brain include both invasive and noninvasive techniques. Invasive technique includes chemical or osmotic opening of BBB while non-invasive technique includes enhanced transcellular transport by modifying the drug to increase their lipid solubility, inhibition of efflux transporters, use of chimeric peptides, trojan horse approach, intranasal delivery and use of transport or carrier systems.The non-invasive carrier system-based strategy utilises delivery of drugs to brain tumors using nano-sized particle systems and this strategy found to have significant potential in improved therapy of brain disorders. Nanoparticle delivery systems can camouflage their cargoes to the brain and can provide sustained release of therapeutic molecules inside the brain resulting in a longer half-life, protection against environmental conditions, and reduced toxicities. Studies comprising direct as well as intravenous administration of nanoparticles loaded with therapeutic agents into the brain have shown promise in the treatment of brain cancers. But, complex synthesis procedures, low biocompatibility and biodegradability, and toxicity problems of nanoparticle delivery systems have raised concerns for their clinical development.
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