Lipids have been well known for decades for contributing to the greater bioavailability of their carrier drug molecules. Especially those drug candidates that have a greater problem of either struggling in their solubility in polar solvents and/or facing first-pass metabolism often become the ideal candidates for lipid-based drug delivery systems. Anti-malarial drugs are among those candidates that too face such challenges, and hence this research review is conducted to touch base on the main aim of formulations to enhance their oral bioavailability, especially where there is a history of first-pass effect or enzymatic drug degradation before the drug reaches the site of absorption or therapeutic action. The application of lipids as one of the prime formulation approaches is believed to be a highly promising concept. Lipoidal-based drug delivery systems are one of the best and most reliable formulation approaches to counter the challenges of properties such as aqueous solubility and bioavailability of lipophilic drug molecules. Lipoidal and lipid-based formulations can be engineered to meet a complete range of product needs, especially by route of administration, disease indications, toxicity, cost considerations, and product stability. When we investigate anti-malarial drugs, they too have poor aqueous solubility and a positive postprandial food effect, making them ideal candidates for lipid-based drug delivery in order to attain increased oral bioavailability. This review covers the various stages of how a drug-micelle conjugate gets emulsified, digested, and absorbed when ingested and explains how it is a very useful tool these days and an ideal delivery system for, especially, drugs of the malaria class. The review also captures the various factors affecting the physical properties of the drug-micelle structures.