Nanotechnological advances for the delivery of CNS therapeutics

Adv Drug Deliv Rev. 2012 May 15;64(7):686-700. doi: 10.1016/j.addr.2011.10.007. Epub 2011 Nov 7.


Effective non-invasive treatment of neurological diseases is often limited by the poor access of therapeutic agents into the central nervous system (CNS). The majority of drugs and biotechnological agents do not readily permeate into brain parenchyma due to the presence of two anatomical and biochemical dynamic barriers: the blood-brain barrier (BBB) and blood-cerebrospinal fluid barrier (BCSFB). Therefore, one of the most significant challenges facing CNS drug development is the availability of effective brain targeting technology. Recent advances in nanotechnology have provided promising solutions to this challenge. Several nanocarriers ranging from the more established systems, e.g. polymeric nanoparticles, solid lipid nanoparticles, liposomes, micelles to the newer systems, e.g. dendrimers, nanogels, nanoemulsions and nanosuspensions have been studied for the delivery of CNS therapeutics. Many of these nanomedicines can be effectively transported across various in vitro and in vivo BBB models by endocytosis and/or transcytosis, and demonstrated early preclinical success for the management of CNS conditions such as brain tumors, HIV encephalopathy, Alzheimer's disease and acute ischemic stroke. Future development of CNS nanomedicines need to focus on increasing their drug-trafficking performance and specificity for brain tissue using novel targeting moieties, improving their BBB permeability and reducing their neurotoxicity.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Blood-Brain Barrier / drug effects
  • Blood-Brain Barrier / metabolism
  • Central Nervous System Agents / administration & dosage*
  • Central Nervous System Agents / metabolism
  • Central Nervous System Diseases / drug therapy*
  • Central Nervous System Diseases / metabolism
  • Drug Delivery Systems / methods
  • Drug Delivery Systems / trends*
  • Humans
  • Nanoparticles / administration & dosage*
  • Nanotechnology / methods
  • Nanotechnology / trends*


  • Central Nervous System Agents