Quantitative analysis of the brain-targeted delivery of drugs and model compounds using nano-delivery systems

Luba Kozlovskaya, David Stepensky

Research output: Contribution to journalReview articlepeer-review

35 Scopus citations


The blood-brain barrier (BBB) prevents drugs' permeability into the brain and limits management of brain diseases. Specialized drug delivery systems (DDSs) are utterly required to overcome this barrier and to achieve efficient delivery of therapeutic agents to the brain. For this purpose, drug-encapsulating nanoparticles or vesicles, drug conjugates and other types of DDSs are being developed by many research groups worldwide. However, efficiency of the brain drug/DDS delivery and targeting is usually presented in indirect and vague form and it is hard to quantitatively estimate it based on the reported data. We searched for the scientific papers that were published in1970-2012 that reported deliveryofdrugsor model compounds to the brain following systemic administration of DDSs via parenteral routes and contained quantitative data on brain drug/DDS delivery and targeting efficiency. We identified 123 publications that matched the search criteria and analyzed their experimental settings, formulation types, analytical methods, and the claimed efficiencies of drug/DDS brain targeting (brain/plasma or brain/tissue concentration ratios) and brain accumulation (% of the administered dose that accumulated in the brain). Based on the outcomes of this analysis, we describe the major research trends, discuss the efficiencies of the different drug/DDS brain targeting approaches, and provide recommendations for quantitative assessment of brain-targeting DDSs in the appropriately designed studies.

Original languageEnglish
Pages (from-to)17-23
Number of pages7
JournalJournal of Controlled Release
Issue number1
StatePublished - 1 Jan 2013


  • Brain drug delivery and targeting
  • Drug conjugates
  • Liposomes
  • Nano-drug delivery systems
  • Nanoparticles

ASJC Scopus subject areas

  • Pharmaceutical Science


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