Cancer is one of the most deadly global diseases, with over 10 million new cases annually. Despite progress in comprehending tumor biology and treatment modalities, obstacles such as multidrug resistance (MDR), aberrant tumor vasculature, and elevated interstitial fluid pressure impede therapeutic effectiveness. Multidrug resistance (MDR), marked by the overexpression of drug-efflux proteins in neoplastic cells, considerably diminishes drug efficacy. Nanotechnology has emerged as a promising approach to overcome these limitations by enabling targeted drug delivery and minimizing side effects. Nanoparticles (NPs), ranging in size from 10 to 1000 nm, improve drug solubility, enhance circulation time, and facilitate tumor accumulation via the Enhanced Permeability and Retention (EPR) effect. They allow controlled drug release, intracellular targeting through endocytosis, and resistance to efflux-mediated drug resistance. Various nanoparticle types include lipid-based systems like liposomes, solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs), and non-lipid systems like ceramic and magnetic nanoparticles. Liposomes are approved for cancer therapy and encapsulate drugs, reducing toxicity and increasing efficacy. Nanocapsules offer high drug-loading capacity and stability, making them suitable for theranostic applications. Developing biocompatible, biodegradable materials such as PLGA (poly-lactide-co-glycolide) enhances the potential of nanoparticulate systems. These systems enable targeted delivery of novel chemotherapeutics, such as pyridine-based compounds, optimizing efficacy while minimizing side effects. Nanotechnology-driven therapies are revolutionizing cancer treatment by addressing critical challenges in drug delivery, offering hope for improved therapeutic outcomes and reduced patient burden.