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a method of targeted drug delivery of an effective amount of an agent, or a pharmaceutical acceptable carrier comprising an agent, to a target site that is protected by a specific blood-tissue barriers like e.g., the CNS, the blood-brain barrier (BBB), the retina and the testes is provided wherein: a) the agent or the pharmaceutical acceptable carrier is conjugated to a ligand, that facilitates the specific binding to and internalization by an internalizing GSH uptake receptor of the target site, thereby forming the conjugate as defined above
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