The book delves into the intricate realm of pharmacokinetics and pharmacodynamics as they apply to modern advancements in drug delivery systems. It offers a comprehensive exploration of novel drug delivery methods, with a particular focus on nanoparticles and nanocarriers. The absorption, distribution, metabolism, and excretion processes of nanoparticles are extensively examined. It also covers various evaluation models, spanning from preclinical to clinical, aimed at assessing the effectiveness and safety of nanoparticles in drug delivery. It also covers the integration of Artificial Intelligence and Machine Learning in pharmacokinetics and pharmacodynamics, showcasing how these cutting-edge approaches can enhance our understanding of drug behavior and optimize therapeutic outcomes. It serves as a comprehensive guide, highlighting the fusion of traditional pharmacological concepts with contemporary drug delivery systems and innovative technologies, all in the pursuit of refining medical treatments and patient care and is a valuable resource for academicians, researchers, and pharmacologists.