At present, the aetiologies of many neurological and neurodegenerative diseases are unknown. However, emergence of a better understanding of these diseases, at both cellular and molecular levels, opens up the possibility of replacement therapies. The presence of the blood-brain barrier complicates the delivery of molecules to the central nervous system. Numerous attempts have been made to bypass this barrier either by delivering the drugs directly into the brain or by transplanting cells to produce the missing molecules in situ. This review explores several methods for delivering bioactive molecules into the CNS, including the use of permeabilizers, osmotic pumps, slow polymer release systems and transplantation of cells with or without the use of the encapsulation technology.