Lipid Nanoparticles: A Novel Approach for Brain Targeting

Pharm Nanotechnol. 2018;6(2):81-93. doi: 10.2174/2211738506666180611100416.


Background: Brain is a delicate organ, separated from general circulation and is characterized by the presence of relatively impermeable Blood Brain Barrier (BBB). The BBB maintains homeostasis in the brain thus restricting the entrance of foreign bodies and several molecules from reaching the brain. As a result several promising molecules do not reach the target site and fail to produce in vivo response. Nevertheless, lipid nanoparticles are taken up readily by the brain because of their lipophilic nature. The bioacceptable and biodegradable nature of lipid nanoparticles makes them less toxic and suited for brain targeting.

Objective: In the present review the BBB, mechanism of transport across the BBB, strategies to bypass the blood-brain barrier have been presented. The aptness of lipid nanoparticles for brain targeting has been highlighted. The proposed mechanism of uptake of the lipid nanoparticles, methods of prolonging the plasma retention and various methods of preparation for formulation of effective delivery systems for brain targeting have been included and dealt in this review.

Conclusion: Lipid based formulations can be designated as the current and future generation of drug delivery systems as these possess tremendous potential to bypass BBB and reach the target site due to their small size and ability to dodge the reticular endothelial system. However, these nanostructures need to be investigated intensively to successfully reach the clinical trials stage.

Keywords: Blood brain barrier; CNS delivery; NLCs; PLNs; solid lipid nanoparticles; targeting strategies..

Publication types

  • Review

MeSH terms

  • Animals
  • Brain / anatomy & histology
  • Brain / metabolism*
  • Brain Diseases / drug therapy
  • Drug Delivery Systems*
  • Humans
  • Lipids / administration & dosage*
  • Lipids / chemistry
  • Nanoparticles / administration & dosage*
  • Nanoparticles / chemistry
  • Particle Size
  • Surface Properties


  • Lipids