The most important function of the blood-retinal barrier (BRB) is maintenance of the homeostasis of the retina environment by separating the retina from the systemic blood circulation. The organization of the BRB is such that the retina is protected from blood-borne compounds, since a strict homeostasis of the neuronal environment and an intact barrier are essential for optimal retina functioning. For treatment of diseases involving the retina, drugs must pass the BRB in a significant amount to have therapeutic effect. Drug entry into the retina, must take into account the plasma concentration profile of the drug, the volume of its distribution, the rate of metabolism of the drug, its plasma protein binding and the relative permeability of the BRB for that drug. All parameters affect the therapeutic efficacy of the drug and are also relevant for potential side effects.In order to obtain therapeutic drug concentrations within the retina, several drug delivery strategies are under current investigation, opening new perspectives for more efficient management of retinal disease.
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