Benzimidazole derivatives are a privileged heterocyclic scaffold with well-established pharmacological activities, including antimicrobial, antiviral, and anticancer properties. Despite their therapeutic promise, many benzimidazole compounds face challenges such as poor aqueous solubility, limited bioavailability, and off-target toxicity, which hinder their clinical translation. Recent advances in nanotechnology have provided innovative solutions to these limitations through the development of benzimidazole-loaded nanoparticles. Nanoparticle-based formulations improve the solubility, stability and pharmacokinetic profile of benzimidazoles while enabling targeted and sustained delivery to tumor tissues. This review provides a comprehensive analysis of the emerging role of benzimidazole-loaded nanoparticles in drug delivery and cancer therapy. It covers the pharmacological significance of benzimidazoles, nanocarrier platforms, targeting mechanisms, preclinical evidence, clinical outlook, challenges, and future perspectives. Emphasis is placed on how nanotechnology enhances the therapeutic performance of benzimidazoles through improved bioavailability, tumor targeting via passive and active strategies, and controlled drug release.