TY - JOUR
T1 - Quantitative analysis of the brain-targeted delivery of drugs and model compounds using nano-delivery systems
AU - Kozlovskaya, Luba
AU - Stepensky, David
N1 - Funding Information:
This study was supported by the Israel Science Foundation grant No 973/11 . The authors have no conflicts of interest that are directly relevant to the content of this study. We thank Dr. Arkady Bolotin (Department of Health Systems Management, Ben-Gurion University of the Negev) for his help in preparation of Fig. 4 .
PY - 2013/1/1
Y1 - 2013/1/1
N2 - 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.
AB - 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.
KW - Brain drug delivery and targeting
KW - Drug conjugates
KW - Liposomes
KW - Nano-drug delivery systems
KW - Nanoparticles
UR - http://www.scopus.com/inward/record.url?scp=84885145148&partnerID=8YFLogxK
U2 - 10.1016/j.jconrel.2013.06.028
DO - 10.1016/j.jconrel.2013.06.028
M3 - Review article
C2 - 23831053
AN - SCOPUS:84885145148
SN - 0168-3659
VL - 171
SP - 17
EP - 23
JO - Journal of Controlled Release
JF - Journal of Controlled Release
IS - 1
ER -