Context: Delivery of a drug into the central nervous system (CNS) is considered difficult. Most of the drugs discovered over the past decade are biological, which are high in molecular weight and polar in nature. The delivery of such drugs across the blood-brain barrier presents problems.
Objective: This review discusses some of the options available to reach the CNS by systemic route. The focus is mainly on the recent developments in systemic delivery of a drug to the CNS.
Materials and methods: Databases such as Scopus, Google scholar, Science Direct, SciFinder and online journals were referred for preparing this article including 89 references.
Results: There are at least nine strategies that could be adopted to achieve the required drug concentration in the CNS.
Conclusion: The recent developments in drug delivery are very promising to deliver biologicals into the CNS.
Keywords: Blood–brain barrier; Trojan; central nervous system; chimeric proteins; peptidomimetics.