Ligand-targeted liposome design: challenges and fundamental considerations

Trends Biotechnol. 2014 Jan;32(1):32-45. doi: 10.1016/j.tibtech.2013.09.007. Epub 2013 Nov 6.


Nanomedicine, particularly liposomal drug delivery, has expanded considerably over the past few decades, and several liposomal drugs are already providing improved clinical outcomes. Liposomes have now progressed beyond simple, inert drug carriers and can be designed to be highly responsive in vivo, with active targeting, increased stealth, and controlled drug-release properties. Ligand-targeted liposomes (LTLs) have the potential to revolutionize the treatment of cancer. However, these highly engineered liposomes generate new problems, such as accelerated clearance from circulation, compromised targeting owing to non-specific serum protein binding, and hindered tumor penetration. This article highlights recent challenges facing LTL strategies and describes the advanced design elements used to circumvent them.

Keywords: EPR effect; PEGylation; active targeting; ligand-targeted liposomes; liposomal drug delivery; liposome stealth.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents
  • Biotechnology*
  • Cell Line, Tumor
  • Drug Delivery Systems*
  • Humans
  • Ligands
  • Liposomes*
  • Mice
  • Nanomedicine*


  • Antineoplastic Agents
  • Ligands
  • Liposomes