Prodrug design has emerged as a dynamic field within pharmaceutical sciences, offering a promising avenue to enhance drug efficacy while mitigating side effects. Defined by Adrien Albert, prodrugs involve modifying parent medications to create inactive precursors that the body converts into active therapeutic agents. Prodrug design aims to optimize medicinal, pharmacokinetic, and pharmacodynamic goals, ultimately improving the therapeutic index and reducing toxicity. Over the past decade, significant strides have been made in prodrug design, particularly in methods enhancing oral bioavailability and targeted delivery to the brain and tumors. Prodrugs offer advantages such as improved pharmacokinetics, targeted drug delivery, reduced toxicity, enhanced stability, and simplified patient compliance. However, challenges such as complex design processes, unpredictable metabolism, and potential side effects must be navigated. Applications of prodrugs span various areas, including oral absorption enhancement, aqueous solubility improvement, lipophilicity alteration, carrier-mediated absorption, and reduction of pain on injection. Prodrugs also show promise in site-selective drug delivery, prolonged drug action, and toxicity reduction. Ongoing research is vital, especially in the early drug development stages, to harness the full potential of prodrug strategies. While prodrugs have become integral to drug design, realistic goals and a continued focus on addressing challenges will contribute to their successful clinical application.