The most adaptable and complicated organ in the human body is the brain. It is protected by the skull bones, a semi-permeable membrane barrier that is highly selective i.e., blood-brain barrier (BBB), and CSF (cerebrospinal fluid). BBB separates the flowing blood from the brain without isolating the brain from other elements of the human body. The blood-brain barrier and also blood-cerebrospinal fluid barrier prevents the entry of lipophilic neurotoxins into the brain. Besides this they only allow selective materials into the brain which maintains homeostasis in the brain, thereby protecting the CNS. There are several techniques to incorporate the drug in the blood brain barrier for the essential treatments of brain and allied diseases which are broadly classified into three basic groups like intensive techniques, non-intensive techniques and miscellaneous techniques and they are further classified with several techniques. Beside this there are some latest approaches like dendrimers, scaffolds, modified nanoparticles also play major role in brain targeted drug delivery. In a nutshell it can said that in modern day there are lots of approaches which are helpful for the researcher to explore the system of drug delivery to the brain.The most adaptable and complicated organ in the human body is the brain. It is protected by the skull bones, a semi-permeable membrane barrier that is highly selective i.e., blood-brain barrier (BBB), and CSF (cerebrospinal fluid). BBB separates the flowing blood from the brain without isolating the brain from other elements of the human body. The blood-brain barrier and also blood-cerebrospinal fluid barrier prevents the entry of lipophilic neurotoxins into the brain. Besides this they only allow selective materials into the brain which maintains homeostasis in the brain, thereby protecting the CNS. There are several techniques to incorporate the drug in the blood brain barrier for the essential treatments of brain and allied diseases which are broadly classified into three basic groups like intensive techniques, non-intensive techniques and miscellaneous techniques and they are further classified with several techniques. Beside this there are some latest approaches like dendrimers, scaffolds, modified nanoparticles also play major role in brain targeted drug delivery. In a nutshell it can said that in modern day there are lots of approaches which are helpful for the researcher to explore the system of drug delivery to the brain.