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Over the last few decades, targeted drug delivery strategies have shown promising applications in the pharmaceutical industry, and it can overcome the downfall of conventional drug delivery systems. Targeted drug delivery approaches involve effective and selective localization of pharmacologically active moiety at preselected target site in therapeutic concentrations, which exhibit various advantages, such as reducing the side effects and toxicity of the drug, improving drug bioavailability, and maximizing the therapeutic drug index. Thus, this chapter explains the passive and active targeted drug delivery strategies and also highlights the enhanced permeation and retention aspects.