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A comprehensive insight on ocular pharmacokinetics

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Abstract

The eye is a distinctive organ with protective anatomy and physiology. Several pharmacokinetics compartment models of ocular drug delivery have been developed for describing the absorption, distribution, and elimination of ocular drugs in the eye. Determining pharmacokinetics parameters in ocular tissues is a major challenge because of the complex anatomy and dynamic physiological barrier of the eye. In this review, pharmacokinetics of these compartments exploring different drugs, delivery systems, and routes of administration is discussed including factors affecting intraocular bioavailability. Factors such as precorneal fluid drainage, drug binding to tear proteins, systemic drug absorption, corneal factors, melanin binding, and drug metabolism render ocular delivery challenging and are elaborated in this manuscript. Several compartment models are discussed; these are developed in ocular drug delivery to study the pharmacokinetics parameters. There are several transporters present in both anterior and posterior segments of the eye which play a significant role in ocular pharmacokinetics and are summarized briefly. Moreover, several ocular pharmacokinetics animal models and relevant studies are reviewed and discussed in addition to the pharmacokinetics of various ocular formulations.

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Acknowledgments

This article has been supported by NIH R01EY09171 and R01EY10659.

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  1. Vivek Agrahari

    Present address: Bayer HealthCare LLC, Shawnee, KS, 66216, USA

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  1. Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City, 2464 Charlotte Street, Kansas City, MO, 64108, USA

    Vibhuti Agrahari, Abhirup Mandal, Vivek Agrahari, Hoang M. Trinh, Mary Joseph, Animikh Ray, Ranjana Mitra, Dhananjay Pal & Ashim K. Mitra

  2. Faculty of Pharmacy, University of Algiers, Algiers, Algeria

    Hicheme Hadji

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Agrahari, V., Mandal, A., Agrahari, V. et al. A comprehensive insight on ocular pharmacokinetics. Drug Deliv. and Transl. Res. 6, 735–754 (2016). https://doi.org/10.1007/s13346-016-0339-2

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