This review discusses the use of lipid-based nanoparticles (LNPs) in delivering bioactive compounds to improve therapeutic efficacy. Bioactive compounds, such as paclitaxel, curcumin, rhodomyrtone, quercetin, kaempferol, resveratrol, epigallocatechin-3-gallate, silymarin, and oridonin, have shown significant therapeutic potential but are often limited by their solubility, bioavailability, and stability. Nanotechnology, particularly LNPs, has been developed to address these limitations by enhancing the physicochemical properties and pharmacokinetic profiles of these compounds. LNPs can encapsulate both hydrophilic and hydrophobic bioactive compounds, providing controlled release, increased bioavailability, and enhanced therapeutic activity. The review highlights the fabrication methods, advantages, and clinical applications of LNPs for various bioactive compounds, emphasizing their potential in improving the therapeutic efficacy of natural bioactive compounds. Safety considerations and the challenges associated with the use of LNPs are also discussed.This review discusses the use of lipid-based nanoparticles (LNPs) in delivering bioactive compounds to improve therapeutic efficacy. Bioactive compounds, such as paclitaxel, curcumin, rhodomyrtone, quercetin, kaempferol, resveratrol, epigallocatechin-3-gallate, silymarin, and oridonin, have shown significant therapeutic potential but are often limited by their solubility, bioavailability, and stability. Nanotechnology, particularly LNPs, has been developed to address these limitations by enhancing the physicochemical properties and pharmacokinetic profiles of these compounds. LNPs can encapsulate both hydrophilic and hydrophobic bioactive compounds, providing controlled release, increased bioavailability, and enhanced therapeutic activity. The review highlights the fabrication methods, advantages, and clinical applications of LNPs for various bioactive compounds, emphasizing their potential in improving the therapeutic efficacy of natural bioactive compounds. Safety considerations and the challenges associated with the use of LNPs are also discussed.