Document Detail


Strategies for therapy of retinal diseases using systemic drug delivery: relevance of transporters at the blood-retinal barrier.
MedLine Citation:
PMID:  22035231     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
There is an increasing need for managing rapidly progressing retinal diseases because of the potential loss of vision. Although systemic drug administration is one possible route for treating retinal diseases, retinal transfer of therapeutic drugs from the circulating blood is strictly regulated by the blood-retinal barrier (BRB). AREAS COVERED: This review discusses the constraints and challenges of drug delivery to the retina. In addition, this article discusses the properties of drugs and the conditions of the BRB that affect drug permeability. The reader will gain insights into the strategies for developing therapeutic drugs that are able to cross the BRB for treating retinal diseases. Further, the reader will gain insights into the role of BRB physiology including barrier functions, and the effect of influx and efflux transporters on retinal drug delivery. EXPERT OPINION: When designing and selecting optimal drug candidates, it's important to consider the fact that they should be recognized by influx transporters and that efflux transporters at the BRB should be avoided. Although lipophilic cationic drugs are known to be transported to the brain across the blood-brain barrier, verapamil transport to the retina is substantially higher than to the brain. Therefore, lipophilic cationic drugs do have a great ability to increase influx transport across the BRB.
Authors:
Ken-ichi Hosoya; Masatoshi Tomi; Masanori Tachikawa
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Review     Date:  2011-10-29
Journal Detail:
Title:  Expert opinion on drug delivery     Volume:  8     ISSN:  1744-7593     ISO Abbreviation:  Expert Opin Drug Deliv     Publication Date:  2011 Dec 
Date Detail:
Created Date:  2011-11-21     Completed Date:  2012-03-08     Revised Date:  2013-05-20    
Medline Journal Info:
Nlm Unique ID:  101228421     Medline TA:  Expert Opin Drug Deliv     Country:  England    
Other Details:
Languages:  eng     Pagination:  1571-87     Citation Subset:  IM    
Affiliation:
University of Toyama, Graduate School of Medicine and Pharmaceutical Sciences, Department of Pharmaceutics, 2630, Sugitani, Toyama 930 0194, Japan. hosoyak@pha.u-toyama.ac.jp
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MeSH Terms
Descriptor/Qualifier:
Animals
Blood-Retinal Barrier / metabolism*
Drug Administration Routes
Humans
Hydrophobic and Hydrophilic Interactions
Membrane Transport Proteins / metabolism*
Permeability
Retinal Diseases / drug therapy*,  metabolism
Chemical
Reg. No./Substance:
0/Membrane Transport Proteins

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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