Nanostructured lipid carriers (NLCs) have emerged as a promising drug delivery platform in cancer therapy, offering advantages such as enhanced drug solubility, stability, and controlled release. Recent efforts have focused on utilizing NLCs for passive and active tumor targeting to improve therapeutic outcomes. This review provides a comprehensive analysis of the role of NLCs in cancer therapy, with particular emphasis on their application in passive and active targeting strategies for precision oncology. Relevant studies were selected from recent literature, focusing on NLC formulation, targeting approaches, and therapeutic applications. NLCs enhance tumor-specific drug delivery through passive targeting via the enhanced permeability and retention (EPR) effect and active targeting via ligand-mediated mechanisms. Lymphatic-targeting NLCs enable improved drug delivery to metastatic niches, while stimuli-responsive NLCs facilitate site-specific release under tumor-associated conditions (e.g., pH, enzymatic activity, redox gradients). Advances in lipid composition, surfactant systems, and conjugation strategies significantly influence drug loading (DL), biodistribution, therapeutic efficacy, and clinical translation across various malignancies. NLCs represent a versatile and adaptable platform for precision cancer therapy. Continued optimization of formulation parameters, functionalization strategies, and clinical translation pathways is essential to fully realize their potential in targeted oncology applications.