In the past few years, significant progress has been made in the field of drug delivery, propelled by emerging novel technologies. Advances in molecular pharmacology, coupled with an enhanced comprehension of disease mechanisms, have underscore the importance of selectively addressing cells implicated in the onset and advancement of diseases. This becomes especially critical in the case of life-threatening conditions, where therapeutic substances, frequently linked to various side effects, require accurate targeting of tissues to reduce overall systemic impact. Recent developments in nanocarrier technology employ sophisticated approaches to enhance targeted drug delivery, optimizing therapeutic effectiveness while minimizing non-specific accumulation in the body. The primary goal of designing nanoscale drug carriers is to enhance their therapeutic potential by improving efficacy and safety. Nanocarriers typically range in diameter from 1 to 100 nm and can be tailored in terms of size, shape, and surface characteristics to interact effectively with biological tissues and cells. Therefore, nanocarrier-drug formulations demonstrate superior attributes compared to other traditional drug delivery systems, showcasing improved performance, precision, and efficacy. These systems incorporate nanomaterials or miniaturized devices with multifunctional components, characterized by biocompatibility, biodegradability, and high viscoelasticity, thereby extending their circulating half-life. Consequently, they play a crucial role in disease management and treatment. This chapter provides the technological progress in drug delivery systems and discusses their therapeutic applications, addressing associated challenges and future perspectives to enhance performance and usability.