The Emerging Significance of Drug Transporters and Metabolizing Enzymes to Ophthalmic Drug Design

  • Mayssa Attar
  • Jie Shen
Part of the Ophthalmology Research book series (OPHRES)


Ophthalmic drugs typically achieve less than 10% ocular bioavailability. A drug applied to the surface of the eye may cross ocular–blood barriers, where it may encounter cellular transporters and metabolizing enzymes, before it is distributed to the site of action. Characterization of ocular membrane transporters, enzyme systems and their respective substrate selectivity has provided new insight into the roles these proteins may play in ocular drug delivery and distribution. Altered drug transport and metabolism have been proposed to contribute to a number of ocular disease processes including inflammation, glaucoma, cataract, dry eye and neurodegeneration. With the development of more-sensitive technologies, ocular transport and enzyme systems will continue to be better characterized, and their properties will become an integral consideration in drug design and development.


Eye disease can profoundly impact a patient's quality of life. As the population of the...


Retinal Pigment Epithelium Ocular Tissue Pseudoxanthoma Elasticum Primary Congenital Glaucoma Diallyl Sulfide 
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Copyright information

© Humana Press, a part of Springer Science + Business Media, LLC 2008

Authors and Affiliations

  • Mayssa Attar
    • 1
  • Jie Shen
    • 1
  1. 1.Department of Pharmacokinetics and Drug MetabolismAllergan Inc.IrvineCA

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