This chapter discusses the evolving field of targeted drug delivery systems (TDDS) and drug delivery systems (DDS) focusing on strategies to enhance the solubility and targeted delivery of insoluble pharmaceutical compounds. Various techniques are explored including changes in pH and salt development, polymeric micelles, nanonization, liposomes, solid lipid nanoparticles, cocrystal preparation, and dendrimers. These strategies aim to overcome challenges such as poor solubility, rapid clearance, and limited bioavailability of drugs, ultimately improving therapeutic efficacy while reducing adverse effects. Additionally, tissue-specific selective drug transporting methods are highlighted, emphasizing the significance of tailored approaches for specific diseases. The chapter concludes by underscoring the significance of continued advancements in technologies related to drug delivery and their potential for novel therapeutic applications, as well as the significance of understanding receptor-ligand biology in translating targeted systems into clinical practice. Overall, the chapter provides a comprehensive overview of existing tactics and potential future prospects in the area of pharmaceuticals delivery, emphasizing the need for precision medicine approaches to improve patient outcomes.