Mannosylerythritol lipids (MELs) have attracted particular interest of medical, pharmaceutical, and cosmetic fields, due to their specific characteristics, including non-toxicity, easy biodegradability, and environmental compatibility. Therefore, this review aims to highlight recent findings on MEL biological properties, focusing on issues related to therapeutic applications. Among the main findings is that MELs can play a fundamental role due to their antimicrobial properties against several nosocomial pathogen microorganisms. Other remarkable biological properties of MELs are related to skincare, as antiaging (active agent), and in particular on recover of skin cells that were damaged by UV radiation. MEL is also related to the increased efficiency of DNA transfection in liposome systems. Regarding the health field, these glycolipids seem to be associated with disturbance in the membrane composition of cancerous cells, increasing expression of genes responsible for cytoplasmic stress and apoptosis. Moreover, MELs can be associated with nanoparticles, as a capping agent, also acting to increase the solubility and cytotoxicity of them. Furthermore, the differences in the chemical structure of MEL could improve and expand their biochemical diversity and applications. Such modifications could change their interfacial properties and, thus, reduce the surface tension value, enhance the solubility, lower critical micelle concentrations, and form unique self-assembly structures. The latest is closely related to molecular recognition and protein stabilization properties of MEL, that is, essential parameters for their effective cosmetical and pharmaceutical effects. Thus, this current research indicates the huge potential of MEL for use in biomedical formulations, either alone or in combination with other molecules.