Designing therapeutic payloads to deliver drug molecules to the desired target site is challenging and requires effective, stable, and safe delivery systems in cancer therapy. Lipid-based nanocarriers have gained substantial interest in preclinical and clinical studies in anticancer drugs, leveraging their potential for drug delivery over the last few decades. While lipid-based nanocarrier technology has achieved some commercial success in different therapeutics and vaccines, challenges persist in their design, development, and quality control in large-scale manufacturing, most notably a lack of robust and scalable lipid-based nanocarrier synthesis and formulation for chemotherapy. To overcome these limitations, it is crucial to understand the role of lipids and other constituents that are utilized in lipid-based nanocarrier synthesis. Along with the compositions of lipid-based nanocarriers, their preparation methods also play a critical role. The structural design of lipid-based nanocarriers aims to impart the desired physicochemical properties, stability, bioavailability, safety, and efficacy of the drug-loaded lipid-based nanocarriers. Initially, this review provides a brief overview of the classification of lipids and other essential components used in the preparation of lipid-based nanocarriers. We then examine critical formulation parameters, including composition ratios, physicochemical characteristics, and preparation methods. We also include the recent progress of cancer nanomedicine and clinical trials, regulatory approval, and future direction to improve the delivery efficiency of lipid-based nanocarriers in cancer nanomedicine. Finally, we summarize the formulation of five distinct types of lipid-based nanocarriers employed for anticancer drug delivery and draw a connection between these formulations and the development of mRNA-based lipid nanoparticles (LNPs).
