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Advanced drug delivery systems employing biomaterial-based approaches have revolutionized modern medicine by enabling targeted therapy with enhanced efficacy and reduced side effects. Biomaterials such as polymeric nanoparticles, liposomes, hydrogels, and micelles serve as carriers or scaffolds to deliver drugs selectively to diseased tissues or cells. This review explores the types of biomaterials used, their advantages in targeted drug delivery, and applications in cancer treatment, chronic diseases, and regenerative medicine. Despite challenges in optimizing targeting efficiency and ensuring biocompatibility, biomaterial-based drug delivery systems hold promise for personalized medicine and improved patient outcomes.